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Chemistry

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Also known as: 2,6-diisopropylphenol, 2078-54-8, Diprivan, Disoprofol, Disoprivan, Fresofol
Molecular Formula
C12H18O
Molecular Weight
178.27  g/mol
InChI Key
OLBCVFGFOZPWHH-UHFFFAOYSA-N
FDA UNII
YI7VU623SF

Propofol
An intravenous anesthetic agent which has the advantage of a very rapid onset after infusion or bolus injection plus a very short recovery period of a couple of minutes. (From Smith and Reynard, Textbook of Pharmacology, 1992, 1st ed, p206). Propofol has been used as ANTICONVULSANTS and ANTIEMETICS.
Propofol is a General Anesthetic. The physiologic effect of propofol is by means of General Anesthesia.
1 2D Structure

Propofol

2 Identification
2.1 Computed Descriptors
2.1.1 IUPAC Name
2,6-di(propan-2-yl)phenol
2.1.2 InChI
InChI=1S/C12H18O/c1-8(2)10-6-5-7-11(9(3)4)12(10)13/h5-9,13H,1-4H3
2.1.3 InChI Key
OLBCVFGFOZPWHH-UHFFFAOYSA-N
2.1.4 Canonical SMILES
CC(C)C1=C(C(=CC=C1)C(C)C)O
2.2 Other Identifiers
2.2.1 UNII
YI7VU623SF
2.3 Synonyms
2.3.1 MeSH Synonyms

1. 2,6 Diisopropylphenol

2. 2,6-bis(1-methylethyl)phenol

3. 2,6-diisopropylphenol

4. Aquafol

5. Diprivan

6. Disoprivan

7. Disoprofol

8. Fresofol

9. Ici 35,868

10. Ici 35868

11. Ici-35,868

12. Ici-35868

13. Ici35,868

14. Ici35868

15. Ivofol

16. Propofol Abbott

17. Propofol Fresenius

18. Propofol Mct

19. Propofol Rovi

20. Propofol-lipuro

21. Recofol

2.3.2 Depositor-Supplied Synonyms

1. 2,6-diisopropylphenol

2. 2078-54-8

3. Diprivan

4. Disoprofol

5. Disoprivan

6. Fresofol

7. Diisopropylphenol

8. 2,6-bis(1-methylethyl)phenol

9. Ampofol

10. Rapinovet

11. Phenol, 2,6-bis(1-methylethyl)-

12. 2,6-di(propan-2-yl)phenol

13. Propofolum

14. Recofol

15. Ivofol

16. Propofol-lipuro

17. Pofol

18. Ici 35868

19. 2,6-diisopropyl Phenol

20. Diprifusor

21. Diprofol

22. Propovan

23. Phenol, 2,6-diisopropyl-

24. Diprivan 10

25. Ici-35868

26. Lipuro

27. Nsc 5105

28. Ici 35,868

29. 2,6-bis(propan-2-yl)phenol

30. 2,6-diisopropyl-phenol

31. Ici35,868

32. Mfcd00008885

33. Chembl526

34. Yi7vu623sf

35. Chebi:44915

36. Nsc5105

37. 2,6-di-iso-propylphenol-d18

38. Phenol, 2,6-bis(1-methylethyl)

39. Nsc-5105

40. Ici 35-868

41. Propofolum [latin]

42. Ncgc00015389-08

43. Aquafol

44. Cas-2078-54-8

45. Dsstox_cid_3523

46. Dsstox_rid_77063

47. Dsstox_gsid_23523

48. Diprivan Injectable Emulsion

49. 2,6 Diisopropylphenol

50. Dipravan

51. Propoven

52. Aquafo

53. Propofol Idd-d

54. Diprivan (tn)

55. Smr000059151

56. Ccris 9000

57. Propofol(2,6-diisopropylphenol)

58. Hsdb 7123

59. 2, 6-diisopropylphenol

60. Sr-01000075468

61. Einecs 218-206-6

62. 2,6-bis(isopropyl)phenol

63. Unii-yi7vu623sf

64. Brn 1866484

65. Dds-04f

66. Ghl.pd_mitscher_leg0.558

67. Ai3-26295

68. Propofol Solution

69. Propofol [usan:usp:inn:ban]

70. Propofol (diprivan)

71. Zd-0859

72. Phenol,6-diisopropyl-

73. Propofol [hsdb]

74. Propofol [usan]

75. Propofol [inn]

76. Propofol [jan]

77. Propofol [mi]

78. Propofol [vandf]

79. Prestwick0_000931

80. Prestwick1_000931

81. Prestwick2_000931

82. Prestwick3_000931

83. 2,6-di Isopropyl Phenol

84. Propofol [mart.]

85. 2,6-dipropan-2-ylphenol

86. Biomol-nt_000248

87. Lopac-d126608

88. Propofol [usp-rs]

89. Propofol [who-dd]

90. Diisopropylphenol (related)

91. Propofol (jan/usp/inn)

92. Lopac0_000437

93. Schembl36245

94. Bspbio_000862

95. 4-06-00-03435 (beilstein Handbook Reference)

96. Mls001066348

97. Mls001335999

98. Mls002454360

99. Bidd:gt0436

100. Propofol [green Book]

101. Spectrum1505022

102. Spbio_003031

103. 2,6-diisopropylphenol, 97%

104. Propofol [ep Impurity]

105. Propofol [orange Book]

106. Bpbio1_000950

107. Bpbio1_000969

108. Gtpl5464

109. Phenol,6-bis(1-methylethyl)-

110. Propofol [ep Monograph]

111. Propofol [usp Impurity]

112. Dtxsid6023523

113. Propofol [usp Monograph]

114. Ketafol Component Propofol

115. Propofol 1.0 Mg/ml In Methanol

116. 2,6-diisopropylphenol, >=97%

117. 3f33

118. 3p50

119. Hms1570l04

120. Hms2089o21

121. Hms2094e17

122. Hms2097l04

123. Hms2231e16

124. Hms3259e03

125. Hms3261g16

126. Hms3369i16

127. Hms3714l04

128. Pharmakon1600-01505022

129. Zinc968303

130. Albb-036351

131. Bcp02920

132. Hy-b0649

133. Tox21_110134

134. Tox21_201371

135. Tox21_303225

136. Tox21_500437

137. Ac8633

138. Bdbm50058046

139. Nsc758909

140. Phenol, 2, 6-bis(1-methylethyl)-

141. Akos009159417

142. Tox21_110134_1

143. Ac-2038

144. Am90311

145. Ccg-204529

146. Cs-w020057

147. Db00818

148. Lp00437

149. Nc00449

150. Nsc-758909

151. Sdccgmls-0318084.p029

152. Sdccgsbi-0050422.p002

153. 2,6-diisopropylphenol; Propofol

154. Mls-0318084

155. Ncgc00015389-01

156. Ncgc00015389-02

157. Ncgc00015389-03

158. Ncgc00015389-04

159. Ncgc00015389-05

160. Ncgc00015389-06

161. Ncgc00015389-07

162. Ncgc00015389-09

163. Ncgc00015389-10

164. Ncgc00015389-11

165. Ncgc00015389-14

166. Ncgc00015389-17

167. Ncgc00091538-01

168. Ncgc00091538-02

169. Ncgc00091538-03

170. Ncgc00091538-04

171. Ncgc00091538-05

172. Ncgc00091538-06

173. Ncgc00257228-01

174. Ncgc00260670-01

175. Ncgc00261122-01

176. As-13299

177. Sy013479

178. 2,6-diisopropylphenol, Analytical Standard

179. Bcp0726000298

180. Mls-0318084.p017

181. Ab00513968

182. D0617

183. Eu-0100437

184. C07523

185. D00549

186. Ab00513968-07

187. Ab00513968_08

188. A814898

189. D126608

190. Q422740

191. Q-201631

192. Sr-01000075468-1

193. Sr-01000075468-4

194. Sr-01000075468-6

195. Brd-k82255054-001-03-5

196. Brd-k82255054-001-08-4

197. Propofol, British Pharmacopoeia (bp) Reference Standard

198. Propofol, European Pharmacopoeia (ep) Reference Standard

199. Z1245735300

200. Propofol, United States Pharmacopeia (usp) Reference Standard

201. Propofol, Pharmaceutical Secondary Standard; Certified Reference Material

202. Propofol For Peak Identification, European Pharmacopoeia (ep) Reference Standard

203. Propofol Solution, 1.0 Mg/ml In Methanol, Ampule Of 1 Ml, Certified Reference Material

204. 113981-41-2

2.4 Create Date
2005-03-25
3 Chemical and Physical Properties
Molecular Weight 178.27 g/mol
Molecular Formula C12H18O
XLogP33.8
Hydrogen Bond Donor Count1
Hydrogen Bond Acceptor Count1
Rotatable Bond Count2
Exact Mass178.135765193 g/mol
Monoisotopic Mass178.135765193 g/mol
Topological Polar Surface Area20.2 Ų
Heavy Atom Count13
Formal Charge0
Complexity135
Isotope Atom Count0
Defined Atom Stereocenter Count0
Undefined Atom Stereocenter Count0
Defined Bond Stereocenter Count0
Undefined Bond Stereocenter Count0
Covalently Bonded Unit Count1
4 Drug and Medication Information
4.1 Drug Information
1 of 4  
Drug NameDiprivan
PubMed HealthPropofol (Injection)
Drug ClassesSedative-Hypnotic
Drug LabelFor IV Administration OnlyRx OnlyStrict aseptic technique must always be maintained during handling. Diprivan Injectable Emulsion is a single-use parenteral product which contains 0.005% disodium edetate to inhibit the rate of growth of microorgani...
Active IngredientPropofol
Dosage FormInjectable
RouteInjection
Strength10mg/ml
Market StatusPrescription
CompanyFresenius Kabi Usa

2 of 4  
Drug NamePropofol
PubMed HealthPropofol (Injection)
Drug ClassesSedative-Hypnotic
Drug LabelPropofol injectable emulsion is a sterile, nonpyrogenic emulsion containing 10 mg/mL of propofol suitable for intravenous administration. Propofol is chemically described as 2,6-diisopropylphenol and has a molecular weight of 178.27. The structural a...
Active IngredientPropofol
Dosage FormInjectable
Routeinjection; Injection
Strength10mg/ml
Market StatusTentative Approval; Prescription
CompanyHospira; Teva Pharms Usa; Gensia Sicor Pharms; Baxter Hlthcare; Esi Lederle

3 of 4  
Drug NameDiprivan
PubMed HealthPropofol (Injection)
Drug ClassesSedative-Hypnotic
Drug LabelFor IV Administration OnlyRx OnlyStrict aseptic technique must always be maintained during handling. Diprivan Injectable Emulsion is a single-use parenteral product which contains 0.005% disodium edetate to inhibit the rate of growth of microorgani...
Active IngredientPropofol
Dosage FormInjectable
RouteInjection
Strength10mg/ml
Market StatusPrescription
CompanyFresenius Kabi Usa

4 of 4  
Drug NamePropofol
PubMed HealthPropofol (Injection)
Drug ClassesSedative-Hypnotic
Drug LabelPropofol injectable emulsion is a sterile, nonpyrogenic emulsion containing 10 mg/mL of propofol suitable for intravenous administration. Propofol is chemically described as 2,6-diisopropylphenol and has a molecular weight of 178.27. The structural a...
Active IngredientPropofol
Dosage FormInjectable
Routeinjection; Injection
Strength10mg/ml
Market StatusTentative Approval; Prescription
CompanyHospira; Teva Pharms Usa; Gensia Sicor Pharms; Baxter Hlthcare; Esi Lederle

4.2 Therapeutic Uses

Propofol is indicated for the induction of general anesthesia. It is also indicated for the maintenance of anesthesia utilizing balanced techniques with other appropriate agents such as opioids and inhalation anesthetics.

MICROMEDEX Thomson Health Care. USPDI - Drug Information for the Health Care Professional. 22nd ed. Volume 1. MICROMEDEX Thomson Health Care, Greenwood Village, CO. 2002. Content Reviewed and Approved by the U.S. Pharmacopeial Convention, Inc., p. 2466


Propofol is indicated for the sedation in critically ill patients confined to intensive care units.

MICROMEDEX Thomson Health Care. USPDI - Drug Information for the Health Care Professional. 22nd ed. Volume 1. MICROMEDEX Thomson Health Care, Greenwood Village, CO. 2002. Content Reviewed and Approved by the U.S. Pharmacopeial Convention, Inc., p. 2466


Propofol has successfully controlled seizures in status epilepticus.

Ellenhorn, M.J., S. Schonwald, G. Ordog, J. Wasserberger. Ellenhorn's Medical Toxicology: Diagnosis and Treatment of Human Poisoning. 2nd ed. Baltimore, MD: Williams and Wilkins, 1997., p. 1181


Propofol appears to have significant antiemetic action and is a good choice for sedation or anesthesia in patients at high risk for nausea and vomiting.

Hardman, J.G., L.E. Limbird, P.B., A.G. Gilman. Goodman and Gilman's The Pharmacological Basis of Therapeutics. 10th ed. New York, NY: McGraw-Hill, 2001., p. 345


4.3 Drug Warning

Compromised cardiovascular function may be aggravated by cardiovascular-depressant and hypotensive effects.

MICROMEDEX Thomson Health Care. USPDI - Drug Information for the Health Care Professional. 22nd ed. Volume 1. MICROMEDEX Thomson Health Care, Greenwood Village, CO. 2002. Content Reviewed and Approved by the U.S. Pharmacopeial Convention, Inc., p. 2467


Caution is also recommended in geriatric, debilitated, and/or hypovolemic patients, because they may require lower induction and maintenance doses.

MICROMEDEX Thomson Health Care. USPDI - Drug Information for the Health Care Professional. 22nd ed. Volume 1. MICROMEDEX Thomson Health Care, Greenwood Village, CO. 2002. Content Reviewed and Approved by the U.S. Pharmacopeial Convention, Inc., p. 2468


Substantial decreases in mean arterial pressure and cerebral perfusion may occur in patients with existing impaired cerebral circulation or increased intracranial pressure.

MICROMEDEX Thomson Health Care. USPDI - Drug Information for the Health Care Professional. 22nd ed. Volume 1. MICROMEDEX Thomson Health Care, Greenwood Village, CO. 2002. Content Reviewed and Approved by the U.S. Pharmacopeial Convention, Inc., p. 2468


Rarely, a clinical syndrome including bronchospasm, erythema, and hypotension has occured shortly after administration of propofol, and sequelae including anoxic brain damage and death have been reported. /SRP: May be from metabisulfite./

MICROMEDEX Thomson Health Care. USPDI - Drug Information for the Health Care Professional. 22nd ed. Volume 1. MICROMEDEX Thomson Health Care, Greenwood Village, CO. 2002. Content Reviewed and Approved by the U.S. Pharmacopeial Convention, Inc., p. 2468


For more Drug Warnings (Complete) data for PROPOFOL (17 total), please visit the HSDB record page.


4.4 Drug Indication

Used for induction and/or maintenance of anaesthesia and for management of refractory status epilepticus.


FDA Label


5 Pharmacology and Biochemistry
5.1 Pharmacology

Propofol is a sedative-hypnotic agent for use in the induction and maintenance of anesthesia or sedation. Intravenous injection of a therapeutic dose of propofol produces hypnosis rapidly with minimal excitation, usually within 40 seconds from the start of an injection (the time for one arm-brain circulation).


5.2 MeSH Pharmacological Classification

Anesthetics, Intravenous

Ultrashort-acting anesthetics that are used for induction. Loss of consciousness is rapid and induction is pleasant, but there is no muscle relaxation and reflexes frequently are not reduced adequately. Repeated administration results in accumulation and prolongs the recovery time. Since these agents have little if any analgesic activity, they are seldom used alone except in brief minor procedures. (From AMA Drug Evaluations Annual, 1994, p174) (See all compounds classified as Anesthetics, Intravenous.)


Hypnotics and Sedatives

Drugs used to induce drowsiness or sleep or to reduce psychological excitement or anxiety. (See all compounds classified as Hypnotics and Sedatives.)


5.3 FDA Pharmacological Classification
5.3.1 Active Moiety
PROPOFOL
5.3.2 FDA UNII
YI7VU623SF
5.3.3 Pharmacological Classes
General Anesthetic [EPC]; General Anesthesia [PE]
5.4 ATC Code

N01AX10

S76 | LUXPHARMA | Pharmaceuticals Marketed in Luxembourg | Pharmaceuticals marketed in Luxembourg, as published by d'Gesondheetskeess (CNS, la caisse nationale de sante, www.cns.lu), mapped by name to structures using CompTox by R. Singh et al. (in prep.). List downloaded from https://cns.public.lu/en/legislations/textes-coordonnes/liste-med-comm.html. Dataset DOI:10.5281/zenodo.4587355


N - Nervous system

N01 - Anesthetics

N01A - Anesthetics, general

N01AX - Other general anesthetics

N01AX10 - Propofol


5.5 Absorption, Distribution and Excretion

Absorption

Rapid - time to onset of unconsciousness is 15-30 seconds, due to rapid distribution from plasma to the CNS. Distribution is so rapid that peak plasma concentrations cannot be readily measured. Duration of action is 5-10 minutes.


Route of Elimination

It is chiefly eliminated by hepatic conjugation to inactive metabolites which are excreted by the kidney.


Volume of Distribution

60 L/kg [healthy adults]


Clearance

23 - 50 mL/kg/min

1.6 - 3.4 L/min [70 Kg adults]


The initial apparent volume of distribution is 13 to 76 L/kg.

MICROMEDEX Thomson Health Care. USPDI - Drug Information for the Health Care Professional. 22nd ed. Volume 1. MICROMEDEX Thomson Health Care, Greenwood Village, CO. 2002. Content Reviewed and Approved by the U.S. Pharmacopeial Convention, Inc., p. 2467


Propofol is rapidly and extensively distributed in the body. It crosses the blood-brain barrier quickly, and its short duration of action is due to rapid redistribution from the CNS to other tissues, high metabolic clearance and high lipophilicity.

MICROMEDEX Thomson Health Care. USPDI - Drug Information for the Health Care Professional. 22nd ed. Volume 1. MICROMEDEX Thomson Health Care, Greenwood Village, CO. 2002. Content Reviewed and Approved by the U.S. Pharmacopeial Convention, Inc., p. 2467


Approximately 70% of a dose is excreted in the urine within 24 hours after administration, and 90% is excreted within 5 days. Clearance of propofol ranges from 1.6 to 3.4 liters per minute in healthy 70 kg patients. As the age of the patient increases, total clearance of propofol may decrease. Clearance rates of 1.4 to 2.2 liters per minute in patients 18 to 35 years of age have been reported, in contrast to clearance rates of 1.0 to 1.8 liters per minute in patients 65 to 80 years of age.

MICROMEDEX Thomson Health Care. USPDI - Drug Information for the Health Care Professional. 22nd ed. Volume 1. MICROMEDEX Thomson Health Care, Greenwood Village, CO. 2002. Content Reviewed and Approved by the U.S. Pharmacopeial Convention, Inc., p. 2467


The pharmacokinetics of propofol were best described by a three-compartment model. Weight was found to be a significant covariate for elimination clearance, the two intercompartmental clearances, and the volumes of the central compartment, the shallow peripheral compartment, and the deep peripheral compartment; power functions with exponents smaller than 1 yielded the best results. The estimates of these parameters for a 70-kg adult were 1.44 l/min, 2.25 l/min, 0.92 l/min, 9.3 l, 44.2 l, and 266 l, respectively. For patients older than 60 yr the elimination clearance decreased linearly. The volume of the central compartment decreased with age. For children, all parameters were increased when normalized to body weight. Venous data showed a decreased elimination clearance; bolus data were characterized by increases in the volumes of the central and shallow peripheral compartments and in the rapid distribution clearance (Cl2) and a decrease in the slow distribution clearance (Cl3). Pharmacokinetics of propofol can be well described by a three-compartment model. Inclusion of age and weight as covariates significantly improved the model. Adjusting pharmacokinetics to the individual patient should improve the precision of target-controlled infusion and may help to broaden the field of application for target-controlled infusion systems.

PMID:10719952 Schuttler J, Ihmsen H; Anesthesiology 92 (3): 727-38 (2000)


An iv dose of 14C-propofol (0.47 mg/kg) administered to 6 male volunteers was rapidly eliminated with 88% recovered in the urine in 5 days and <2% in feces. The dose was cleared by metabolism with <0.3% excreted unchanged. The major metabolites were the glucuronic acid conjugate of propofol and the glucuronic acid and sulfate conjugates of its hydroxylated derivative, 2,6-diisopropyl-1,4-quinol. Propofol glucuronide accounted for about 53% of the urinary radioactivity and was the major metabolite in plasma from 30 min post dose. The blood concentration of propofol declined in a biphasic manner from a maximum mean value of 0.44 ug/ml, 2 min after injection. The half-lives of the first and second exponential phases, mean values 5 min and 97 min respectively, varied widely among subjects. A proportion of the dose was cleared slowly, probably due to slow release from less well perfused tissues. Propofol accounted for 94% of the total blood radioactivity at 2 min but only about 6% from 3 to 8 hr post dose. Propofol has a volume of distribution equivalent to about 3 to 4 times body weight, and a mean total body clearance of 2.2 l/min.

PMID:3261062 Simons P, Cockshott I; Xenobiotica 18 (4): 429-40 (1988)


5.6 Metabolism/Metabolites

Hepatically metabolized mainly by glucuronidation at the C1-hydroxyl. Hydroxylation of the benzene ring to 4-hydroxypropofol may also occur via CYP2B6 and 2C9 with subsequent conjugation to sulfuric and/or glucuronic acid. Hydroxypropofol has approximately 1/3 of hypnotic activity of propofol.


Hepatic; rapidly undergoes glucuronide conjugation to inactive metabolites. An unidentified route of extrahepatic metabolism may also exist, suggested by the fact that propofol clearance exceeds estimated hepatic blood flow.

MICROMEDEX Thomson Health Care. USPDI - Drug Information for the Health Care Professional. 22nd ed. Volume 1. MICROMEDEX Thomson Health Care, Greenwood Village, CO. 2002. Content Reviewed and Approved by the U.S. Pharmacopeial Convention, Inc., p. 2467


To determine the cytochrome P450 (CYP) isoforms involved in the oxidation of propofol by human liver microsomes. The rate constant calculated from the disappearance of propofol in an incubation mixture with human liver microsomes and recombinant human CYP isoforms was used as a measure of the rate of metabolism of propofol. The correlation of these rate constants with rates of metabolism of CYP isoform-selective substrates by liver microsomes, the effect of CYP isoform-selective chemical inhibitors and monoclonal antibodies on propofol metabolism by liver microsomes, and its metabolism by recombinant human CYP isoforms were examined. The mean rate constant of propofol metabolism by liver microsomes obtained from 6 individuals was 4.2 (95% confidence intervals 2.7, 5.7) nmol/min/mg protein. The rate constants of propofol by microsomes were significantly correlated with S-mephenytoin N-demethylation, a marker of CYP2B6 (r=0.93, P<0.0001), but not with the metabolic activities of other CYP isoform-selective substrates. Of the chemical inhibitors of CYP isoforms tested, orphenadrine, a CYP2B6 inhibitor, reduced the rate constant of propofol by liver microsomes by 38% (P<0.05), while other CYP isoform-selective inhibitors had no effects. Of the recombinant CYP isoforms screened, CYP2B6 produced the highest rate constant for propofol metabolism (197 nmol/min/nmol P450). An antibody against CYP2B6 inhibited the disappearance of propofol in liver microsomes by 74% /and SRP: reduced in vitro metabolism by blocking CYP 2B6/. Antibodies raised against other CYP isoforms had no effect on the metabolism of propofol. CYP2B6 is predominantly involved in the oxidation of propofol by human liver microsomes.

Oda Y, Hamaoka N; Br J Clin Pharmacol 51 (3): 281-5 (2001


Propofol has known human metabolites that include (2S,3S,4S,5R)-6-[2,6-Di(propan-2-yl)phenoxy]-3,4,5-trihydroxyoxane-2-carboxylic acid and 4-hydroxy-propofol.

S73 | METXBIODB | Metabolite Reaction Database from BioTransformer | DOI:10.5281/zenodo.4056560


5.7 Biological Half-Life

Initial distribution phase t1/2α=1.8-9.5 minutes. Second redistirubtion phase t1/2β=21-70 minutes. Terminal elimination phase t1/2γ=1.5-31 hours.


Terminal elimination half-life is 3 to 12 hours; prolonged administration may result in longer duration.

MICROMEDEX Thomson Health Care. USPDI - Drug Information for the Health Care Professional. 22nd ed. Volume 1. MICROMEDEX Thomson Health Care, Greenwood Village, CO. 2002. Content Reviewed and Approved by the U.S. Pharmacopeial Convention, Inc., p. 2467


...The first-stage elimination half-life (t1/2 beta) of propofol /SRP: administered mixed with lidocaine/ in children was shorter (mean 9.3 +/- 3.8 (s.d.) min) than the values found in adults. This pharmacokinetic alteration may have clinical significance following repeated administration or continuous infusion of propofol.

PMID:2646847 Valtonen M, et al; Acta Anaesthesiol Scand 33 (2): 152-5 (1989)


An intravenous dose of 14C-propofol (0.47 mg/kg) /was/ administered to six male volunteers... . ...The half-lives of the first and second exponential phases, mean values 5 min and 97 min respectively, varied widely among subjects.

PMID:3261062 Simons P, Cockshott I; Xenobiotica 18 (4): 429-40 (1988)


5.8 Mechanism of Action

The action of propofol involves a positive modulation of the inhibitory function of the neurotransmitter gama-aminobutyric acid (GABA) through GABA-A receptors.


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INC","customerCountry":"INDIA","quantity":"761.00","actualQuantity":"761","unit":"KGS","unitRateFc":"189.1","totalValueFC":"145376.1","currency":"USD","unitRateINR":"15863.9","date":"22-Mar-2024","totalValueINR":"12072420","totalValueInUsd":"145376.1","indian_port":"Vizag-RPCIPL SEZ","hs_no":"29071990","bill_no":"1000456","productDescription":"API","marketType":"REGULATED MARKET","country":"UNITED STATES","selfForZScoreResived":"Pharma Grade","supplierPort":"N\/A","supplierAddress":"N\/A","customerAddress":"PLOT NO.B3,B4&B5 PT SIPCOT,INDUSTR"},{"dataSource":"API Import","activeIngredients":"","year":"2024","qtr":"Q2","strtotime":1714588200,"product":"PROPOFOL PH EUR LOT NO: 1000082676 MATERIAL CODE: 4037808","address":"CLARIS CORPORATE HEAD QUARTERS,","city":"ELLISBRIDGE,AHMEDABD,GUJARAT,INDIA","supplier":"BACHEM AG","supplierCountry":"SWITZERLAND","foreign_port":"BASLE","customer":"BAXTER HEALTHCARE CORPORATION","customerCountry":"INDIA","quantity":"1915.20","actualQuantity":"1915.2","unit":"KGS","unitRateFc":"165","totalValueFC":"321173.1","currency":"USD","unitRateINR":"13926","date":"02-May-2024","totalValueINR":"26671075.2","totalValueInUsd":"321173.1","indian_port":"Ahmedabad Air","hs_no":"29071910","bill_no":"3294076","productDescription":"API","marketType":"REGULATED MARKET","country":"SWITZERLAND","selfForZScoreResived":"Pharma Grade","supplierPort":"BASLE","supplierAddress":"HAUPTSTRASSE 144 CH-4416 BUBENDORF, SWITZERLAND, SWITZERLANDSDNF SWITZERLAND","customerAddress":"CLARIS CORPORATE HEAD QUARTERS,"},{"dataSource":"API Import","activeIngredients":"","year":"2024","qtr":"Q2","strtotime":1714588200,"product":"PROPOFOL PH EUR LOT NO: 1000084693 MATERIAL CODE: 4037808","address":"CLARIS CORPORATE HEAD QUARTERS,","city":"ELLISBRIDGE,AHMEDABD,GUJARAT,INDIA","supplier":"BACHEM AG","supplierCountry":"SWITZERLAND","foreign_port":"BASLE","customer":"BAXTER HEALTHCARE CORPORATION","customerCountry":"INDIA","quantity":"1678.08","actualQuantity":"1678.08","unit":"KGS","unitRateFc":"165","totalValueFC":"281408.8","currency":"USD","unitRateINR":"13926","date":"02-May-2024","totalValueINR":"23368942.08","totalValueInUsd":"281408.8","indian_port":"Ahmedabad Air","hs_no":"29071910","bill_no":"3294076","productDescription":"API","marketType":"REGULATED MARKET","country":"SWITZERLAND","selfForZScoreResived":"Pharma Grade","supplierPort":"BASLE","supplierAddress":"HAUPTSTRASSE 144 CH-4416 BUBENDORF, SWITZERLAND, SWITZERLANDSDNF SWITZERLAND","customerAddress":"CLARIS CORPORATE HEAD QUARTERS,"},{"dataSource":"API Import","activeIngredients":"","year":"2024","qtr":"Q2","strtotime":1719167400,"product":"4037808 PROPOFOL LOT NO. 1000083380","address":"GF- 1 , GROUND FLOOR,COMMERCE HOUSE","city":"BUNGALOW ROAD, BODAKDEV AHMEDABAD.","supplier":"BACHEM AG","supplierCountry":"SWITZERLAND","foreign_port":"BASLE","customer":"TROIKAA PHARMACEUTICALS LIMITED","customerCountry":"INDIA","quantity":"170.24","actualQuantity":"170.24","unit":"KGS","unitRateFc":"230","totalValueFC":"40103.3","currency":"USD","unitRateINR":"19562.3","date":"24-Jun-2024","totalValueINR":"3330288.36","totalValueInUsd":"40103.3","indian_port":"Ahmedabad Air","hs_no":"29071990","bill_no":"4154913","productDescription":"API","marketType":"REGULATED MARKET","country":"SWITZERLAND","selfForZScoreResived":"Pharma Grade","supplierPort":"BASLE","supplierAddress":"Hauptstrasse 144 CH-4416 BUBENDORFSDNFSDNF Switzerland","customerAddress":"GF- 1 , GROUND FLOOR,COMMERCE HOUSE"},{"dataSource":"API Import","activeIngredients":"","year":"2024","qtr":"Q2","strtotime":1719253800,"product":"PROPOFOL","address":"140, DAMJI SHAMJI INDL.COMPLEX, 28","city":"ANDHERI [E],MUMBAI \/ MAHARASHTRA","supplier":"BACHEM AG","supplierCountry":"SWITZERLAND","foreign_port":"BASLE","customer":"NEON LABORATORIES","customerCountry":"INDIA","quantity":"121.60","actualQuantity":"121.6","unit":"KGS","unitRateFc":"230","totalValueFC":"29254.3","currency":"USD","unitRateINR":"19978.3","date":"25-Jun-2024","totalValueINR":"2429357.4","totalValueInUsd":"29254.3","indian_port":"Bombay Air","hs_no":"29071990","bill_no":"4175927","productDescription":"API","marketType":"REGULATED MARKET","country":"SWITZERLAND","selfForZScoreResived":"Pharma Grade","supplierPort":"BASLE","supplierAddress":"SUCCURSALE DE VIONNAZ ROUTE DU SIMPLON 22 1895 VIONNAZ SWITZERLANDSDNF SWITZERLAND","customerAddress":"140, DAMJI SHAMJI INDL.COMPLEX, 28"},{"dataSource":"API Import","activeIngredients":"","year":"2024","qtr":"Q2","strtotime":1719426600,"product":"PROPOFOL","address":"NARBAVI, NO.3,LAKSHMANAN STREET,","city":"CHENNAI\/TAMILNADU","supplier":"BACHEM AG","supplierCountry":"SWITZERLAND","foreign_port":"BASEL\/MULHOUSE","customer":"CAPLIN POINT LABORATORIES LIMITED","customerCountry":"INDIA","quantity":"48.64","actualQuantity":"48.64","unit":"KGS","unitRateFc":"230","totalValueFC":"11864.2","currency":"USD","unitRateINR":"20255.6","date":"27-Jun-2024","totalValueINR":"985230.96","totalValueInUsd":"11864.2","indian_port":"Madras Air","hs_no":"29071910","bill_no":"4212968","productDescription":"API","marketType":"REGULATED MARKET","country":"SWITZERLAND","selfForZScoreResived":"Pharma Grade","supplierPort":"BASEL\/MULHOUSE","supplierAddress":"Succursale de VionnazRoute du Simplon 221895 Vionnaz Schweiz SZ","customerAddress":"NARBAVI, NO.3,LAKSHMANAN STREET,"},{"dataSource":"API Import","activeIngredients":"","year":"2024","qtr":"Q3","strtotime":1723055400,"product":"PROPOFOL","address":"Plot No.4C, MN science & technology biotech park phase-I","city":"Hyderabad","supplier":"BACHEM AG","supplierCountry":"SWITZERLAND","foreign_port":"BASLE","customer":"PRATHYAK LABORATORIES PRIVATE LIMITED","customerCountry":"INDIA","quantity":"6.08","actualQuantity":"6.08","unit":"KGS","unitRateFc":"450","totalValueFC":"2787.3","currency":"USD","unitRateINR":"38070","date":"08-Aug-2024","totalValueINR":"231465.6","totalValueInUsd":"2787.3","indian_port":"Hyderabad Air","hs_no":"29071990","bill_no":"4938347","productDescription":"API","marketType":"REGULATED MARKET","country":"SWITZERLAND","selfForZScoreResived":"Pharma Grade","supplierPort":"BASLE","supplierAddress":"SUCCURSALE DE VIONNAZ ROUTE DUSIMPLON 22 1895 VIONNAZSCHWEIZ SWITZERLAND CH","customerAddress":"Plot No.4C, MN science & technology biotech park phase-I"},{"dataSource":"API Import","activeIngredients":"","year":"2024","qtr":"Q3","strtotime":1723141800,"product":"4037808 PROPOFOL 1000091832","address":"GF- 1 , GROUND FLOOR,COMMERCE HOUSE","city":"BUNGALOW ROAD, BODAKDEV AHMEDABAD.","supplier":"BACHEM AG","supplierCountry":"SWITZERLAND","foreign_port":"BASLE","customer":"TROIKAA PHARMACEUTICALS LIMITED","customerCountry":"INDIA","quantity":"97.28","actualQuantity":"97.28","unit":"KGS","unitRateFc":"230","totalValueFC":"23507.1","currency":"USD","unitRateINR":"20066.8","date":"09-Aug-2024","totalValueINR":"1952094.24","totalValueInUsd":"23507.1","indian_port":"Ahmedabad Air","hs_no":"29071990","bill_no":"4961236","productDescription":"API","marketType":"REGULATED MARKET","country":"SWITZERLAND","selfForZScoreResived":"Pharma Grade","supplierPort":"BASLE","supplierAddress":"Succursale de Vionnaz Route du Simplon 22 1895 Vionnaz SchweizSDNF Switzerland","customerAddress":"GF- 1 , GROUND FLOOR,COMMERCE HOUSE"},{"dataSource":"API Import","activeIngredients":"","year":"2024","qtr":"Q3","strtotime":1723401000,"product":"PROPOFOL","address":"Gala No136,1st Flr Building No.5,","city":"MUMBAI","supplier":"BACHEM AG","supplierCountry":"SWITZERLAND","foreign_port":"BASLE","customer":"SAMARTH LIFE SCIENCES PRIVATE LIMITED","customerCountry":"INDIA","quantity":"145.92","actualQuantity":"145.92","unit":"KGS","unitRateFc":"250","totalValueFC":"37164.1","currency":"USD","unitRateINR":"21150","date":"12-Aug-2024","totalValueINR":"3086208","totalValueInUsd":"37164.1","indian_port":"Bombay Air","hs_no":"29071990","bill_no":"5008105","productDescription":"API","marketType":"REGULATED MARKET","country":"SWITZERLAND","selfForZScoreResived":"Pharma Grade","supplierPort":"BASLE","supplierAddress":"HAUPTSTRASSE 144SDNFCH-4416 BUBENDORF SWAZILAND","customerAddress":"Gala No136,1st Flr Building No.5,"},{"dataSource":"API Import","activeIngredients":"","year":"2024","qtr":"Q3","strtotime":1724265000,"product":"PROPOFOL PH EUR LOT NO: 1000095885 MATERIAL CODE: 4037808","address":"CLARIS CORPORATE HEAD QUARTERS,","city":"ELLISBRIDGE,AHMEDABD,GUJARAT,INDIA","supplier":"BACHEM AG","supplierCountry":"SWITZERLAND","foreign_port":"BASLE","customer":"BAXTER HEALTHCARE CORPORATION","customerCountry":"INDIA","quantity":"1763.20","actualQuantity":"1763.2","unit":"KGS","unitRateFc":"165","totalValueFC":"297259.7","currency":"USD","unitRateINR":"14000.3","date":"22-Aug-2024","totalValueINR":"24685240.8","totalValueInUsd":"297259.7","indian_port":"Ahmedabad Air","hs_no":"29071910","bill_no":"5187204","productDescription":"API","marketType":"REGULATED MARKET","country":"SWITZERLAND","selfForZScoreResived":"Pharma Grade","supplierPort":"BASLE","supplierAddress":"HAUPTSTRASSE 144 CH-4416 BUBENDORF, SWITZERLAND, SWITZERLANDSDNF SWITZERLAND","customerAddress":"CLARIS CORPORATE HEAD QUARTERS,"}]
27-Jan-2021
30-Aug-2024
KGS
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Quantity (KGS) & Unit rate (USD/KGS) over time

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FDF Dossiers

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01

  • fda
  • EDQM
  • WHO-GMP

Virtual BoothNaprod is a top player in Oncology & Anesthesia FDF through excellent innovation, discovery of new processes & high-quality production.

Flag India
Digital Content Digital Content

Regulatory Info :

Registration Country : India

Propofol

Brand Name :

Dosage Form : Liquid Injection

Dosage Strength : 10MG/ML

Packaging :

Approval Date :

Application Number :

Regulatory Info :

Registration Country : India

Naprod Life Sciences

02

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BioProcess International
Not Confirmed

PROPOFOL

Brand Name : DIPRIVAN 1%

Dosage Form : EMULSION

Dosage Strength : 10MG/ML

Packaging : 20/ML50ML/100ML

Approval Date :

Application Number : 2018950

Regulatory Info : Prescription

Registration Country : Canada

Aspen API Comapny Banner

03

  • fda
  • EDQM
  • WHO-GMP

Virtual BoothDRL offers a portfolio of products & services, including APIs, CMO services, generics, biosimilars & differentiated formulations.

Flag India
Digital Content Digital Content

Regulatory Info : RX

Registration Country : USA

PROPOFOL

Brand Name : PROPOFOL

Dosage Form : INJECTABLE;INJECTION

Dosage Strength : 10MG/ML

Packaging :

Approval Date : 2018-11-15

Application Number : 205067

Regulatory Info : RX

Registration Country : USA

Dr Reddy Company Banner

04

Actavis Inc

Ireland
BioProcess International
Not Confirmed
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Actavis Inc

Ireland
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BioProcess International
Not Confirmed

PROPOFOL

Brand Name : PROPOFOL

Dosage Form : INJECTABLE;INJECTION

Dosage Strength : 10MG/ML

Packaging :

Approval Date : 2015-12-22

Application Number : 205307

Regulatory Info : DISCN

Registration Country : USA

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05

BioProcess International
Not Confirmed
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BioProcess International
Not Confirmed

Propofol

Brand Name : Propofol

Dosage Form : Propofol 500Mg 50Ml 10 Units Parenteral Use

Dosage Strength : 10 VIALS EV 50 ml 1%

Packaging :

Approval Date :

Application Number :

Regulatory Info :

Registration Country : Italy

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06

BioProcess International
Not Confirmed
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BioProcess International
Not Confirmed

Propofol

Brand Name : Propofol-Lipuro

Dosage Form : Injection/infusion fluid, Emulsion

Dosage Strength : 10 mg/ml

Packaging : The infusion bottle of glass

Approval Date :

Application Number :

Regulatory Info :

Registration Country : Norway

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07

Farbe Firma

India
BioProcess International
Not Confirmed
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Farbe Firma

India
arrow
BioProcess International
Not Confirmed

Propofol

Brand Name :

Dosage Form : Injection

Dosage Strength : 20MG/ML

Packaging :

Approval Date :

Application Number :

Regulatory Info :

Registration Country : India

blank

08

Farmak JSC

Ukraine
BioProcess International
Not Confirmed
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Farmak JSC

Ukraine
arrow
BioProcess International
Not Confirmed

Propofol

Brand Name : Diprofol®EDTA 2%

Dosage Form : Emulsion for Injection

Dosage Strength : 20MG/ML

Packaging : 20ML in Ampoule, 20ML in Vial, 50ML in Vial

Approval Date :

Application Number :

Regulatory Info :

Registration Country : Ukraine

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09

BioProcess International
Not Confirmed
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BioProcess International
Not Confirmed

Propofol

Brand Name : PROPOFOL 1% PS FRESENIUS

Dosage Form : INJ

Dosage Strength : 10mg

Packaging : 10X6mg

Approval Date :

Application Number :

Regulatory Info : Generic

Registration Country : South Africa

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10

BioProcess International
Not Confirmed
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BioProcess International
Not Confirmed

PROPOFOL

Brand Name : PROPOFOL

Dosage Form : INJECTABLE;INJECTION

Dosage Strength : 10MG/ML

Packaging :

Approval Date : 1999-01-04

Application Number : 75102

Regulatory Info : RX

Registration Country : USA

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Europe

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01

AstraZeneca AB

United Kingdom
BioProcess International
Not Confirmed
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AstraZeneca AB

United Kingdom
arrow
BioProcess International
Not Confirmed

propofol

Brand Name : Diprivan

Dosage Form : INJECTION / EMULSION FOR INFUSION

Dosage Strength : 10 MG / ML

Packaging :

Approval Date :

Application Number :

Regulatory Info :

Registration Country : Sweden

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02

BioProcess International
Not Confirmed
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BioProcess International
Not Confirmed

propofol

Brand Name : Propofol-Lipuro

Dosage Form : INJEKTIONSVÄTSKA/INFUSIONSVÄTSKA, EMULSION

Dosage Strength : 10 MG/ML

Packaging :

Approval Date :

Application Number :

Regulatory Info :

Registration Country : Sweden

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03

BioProcess International
Not Confirmed
arrow
arrow
BioProcess International
Not Confirmed

Propofol

Brand Name : Propofol-Lipuro

Dosage Form : Injection/infusion fluid, Emulsion

Dosage Strength : 10 mg/ml

Packaging : The infusion bottle of glass

Approval Date :

Application Number :

Regulatory Info :

Registration Country : Norway

blank

04

BioProcess International
Not Confirmed
arrow
arrow
BioProcess International
Not Confirmed

Propofol

Brand Name : Propofol-Lipuro

Dosage Form : Injection/infusion fluid, Emulsion

Dosage Strength : 10 mg/ml

Packaging : The infusion bottle of glass

Approval Date :

Application Number :

Regulatory Info :

Registration Country : Norway

blank

05

Baxter B.V.

Germany
BioProcess International
Not Confirmed
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Baxter B.V.

Germany
arrow
BioProcess International
Not Confirmed

Propofol

Brand Name : Profast

Dosage Form : Injection/infusion liquid, emulsion

Dosage Strength : 10 mg/ml

Packaging : Vials 10 50ml

Approval Date :

Application Number :

Regulatory Info :

Registration Country : Norway

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06

BioProcess International
Not Confirmed
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BioProcess International
Not Confirmed

propofol

Brand Name : Propolipid

Dosage Form : INJEKTIONS-/INFUSIONSVÄTSKA, EMULSION I

Dosage Strength : 20 MG/ML

Packaging :

Approval Date :

Application Number :

Regulatory Info :

Registration Country : Sweden

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07

BioProcess International
Not Confirmed
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BioProcess International
Not Confirmed

Propofol

Brand Name : Propofol

Dosage Form : Propofol 1.000Mg 100Ml 10 Units Parenteral Use

Dosage Strength : 10 VIALS EV 100 ml 10 mg/ml

Packaging :

Approval Date :

Application Number :

Regulatory Info :

Registration Country : Italy

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08

BioProcess International
Not Confirmed
arrow
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BioProcess International
Not Confirmed

Propofol

Brand Name : Propofol

Dosage Form : Propofol 1.000Mg 50Ml 10 Units Parenteral Use

Dosage Strength : 10 VIALS EV 50 ml 20 mg/ml

Packaging :

Approval Date :

Application Number :

Regulatory Info :

Registration Country : Italy

blank

09

BioProcess International
Not Confirmed
arrow
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BioProcess International
Not Confirmed

Propofol

Brand Name : Propolipid

Dosage Form : Injection/infusion fluid, Emulsion

Dosage Strength : 20 mg/ml

Packaging : Hood glass

Approval Date :

Application Number :

Regulatory Info :

Registration Country : Norway

blank

10

BioProcess International
Not Confirmed
arrow
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BioProcess International
Not Confirmed

Propofol

Brand Name : Propofol

Dosage Form : Propofol 200Mg 20Ml 5 Units Parenteral Use

Dosage Strength : 5 vials 200 mg 20 ml

Packaging :

Approval Date :

Application Number :

Regulatory Info :

Registration Country : Italy

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DATA COMPILATION #PharmaFlow

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Pharma Deals, Investments and M&As in September 2017
In our continuous endeavor to share business intelligence that can help grow your pharmaceutical business, PharmaCompass had introduced PharmaFlow last month — a monthly roundup of deals and investments from across the globe. By tracking investments and M&As in the global pharmaceutical industry, we hope to provide our readers with an insight into the breakthrough technologies and business trends of the future. In September, Teva continued to divest in order to reduce its US$ 35 billion debt burden incurred last year due to the acquisition of the generics division of Allergan. Meanwhile, the world of pharmaceuticals saw deals in the medical devices space, and the Chinese drug industry continued to expand its global footprint. Click here to view the major deals in September 2017 (Excel version available) for FREE! Teva’s disinvestments lead the deals in September Debt-laden Teva Pharmaceuticals, the world’s leading generic drug manufacturer, continued to look for divestiture opportunities and sealed three separate divestments that together fetched US$ 2.48 billion. The Israeli drugmaker, which also got a new CEO (Kåre Schultz) last month, announced it would use the proceeds to repay its term loan debt. Capital Partners Fund VI acquired a portfolio of products from Teva’s global women’s health business, spanning contraception, fertility, menopause and osteoporosis for US$ 703 million in cash. The portfolio of products, marketed and sold outside of the US, includes brands such as Ovaleap, Zoely, Seasonique, Colpotrophine and Actonel. Combined annual net sales of these and other products within this portfolio for 2016 were US$ 258 million. Teva has also entered into an agreement under which Foundation Consumer Healthcare will acquire Plan B One-Step and Teva’s value brands of emergency contraception (Take Action, Aftera, and Next Choice One Dose) for US$ 675 million in cash. Combined annual net sales of Plan B One-Step, Take Action, Aftera, and Next Choice One Dose were US$ 140 million in 2016. Click here to view the major deals in September 2017 (Excel version available) for FREE! Teva also entered into a definitive agreement with CooperSurgical, under which the latter will acquire Paragard (intrauterine copper contraceptive), a product within its global women’s health business, for US$ 1.1 billion cash. Paragard posted revenues of approximately US$ 168 million for the trailing 12 month period ending June 30, 2017. This transaction also includes the sale of Teva’s manufacturing facility in Buffalo, New York, which produces Paragard exclusively.   M&As in the next generation medical devices space NeoTract acquires Teleflex: September also saw the acquisition of NeoTract by Teleflex Incorporated. NeoTract is a privately-held medical device company that has developed and commercialized the US FDA-cleared UroLift System — a novel, minimally invasive technology for treating lower urinary tract symptoms due to benign prostatic hyperplasia, or BPH. Performed primarily through a transurethral outpatient procedure, the UroLift System delivers permanent implants that hold open the urethra, reducing the prostate obstruction without cutting, heating, or removing prostate tissue. Teleflex saw significant potential in NeoTract’s technology and acquired the company in early September, in a transaction valued up to US$ 1.1 billion. Click here to view the major deals in September 2017 (Excel version available) for FREE! Under the terms of the agreement, Teleflex will acquire NeoTract for an upfront cash payment of US$ 725 million, and will pay up to an additional US$ 375 million upon the achievement of certain commercial milestones related to sales through the end of 2020.  In 2016, NeoTract reported 178 percent year-on-year growth as its revenues grew to US$ 51 million compared to approximately US$ 18 million in 2015.  Shandong Weigao acquires Argon Medical Devices: In another major medical device deal announced in September, China’s Shandong Weigao Group Medical Polymer agreed to buy closely held Argon Medical Devices for US$ 850 million. Argon, which posted revenues of US$ 225 million last year, makes devices including biopsy products, drainage catheters and systems that remove blood clots. Once the purchase is complete, Argon will become one of Shandong Weigao’s “core platforms” for overseas expansion.  Chinese companies carry on with their global acquisition spree Shandong Weigao isn’t alone as according to Bloomberg data, Chinese companies had announced US$ 4.3 billion in US health-care deals until September, more than double the US$ 1.9 billion in purchases for the same period in 2016. Chinese deals in Canada, US: In January this year, Chinese conglomerate Sanpower Group had acquired Valeant Pharmaceuticals’ Dendreon cancer business for US$ 819.9 million. Dendreon makes the prostate cancer vaccine — Provenge. In June this year, Chinese contraceptives maker Humanwell Healthcare Group agreed to buy US-based RiteDose for about US$ 605 million by becoming a part of a joint stock company. Fosun resurrects India deal: In September, Shanghai Fosun Pharmaceutical Group resurrected its deal to overcome concerns raised by the Indian government, by scaling down the stake it proposed to purchase in Gland Pharma from 86 percent to 74 percent. Fosun now proposes to pay US$ 1.1 billion for the 74 percent stake. The acquisition will give Fosun access to the Indian drugmaker’s portfolio of generic injectable medicines that are primarily exported to the US. Zai Lab’s US IPO: Last month, China-based Zai Lab — a Chinese biotech focused on oncology, autoimmune and infectious diseases — raised US$ 150 million in its US IPO after the company increased the size of the offering to 8 million shares, from the originally proposed 5.8 million shares. Demand for the shares was strong, and Zai's stock opened 50 percent above the IPO price valuing the company at US$ 1.4 billion. Click here to view the major deals in September 2017 (Excel version available) for FREE!   Aspen acquires another portfolio of drugs from Big Pharma Last year, Italian antitrust authorities fined South Africa-based drugmaker Aspen Pharmacare nearly US$ 5.5 million for halting supplies of several cancer drugs. This was seen as a negotiating tactic designed to hike drug prices by as much as 1,500 percent. The products whose supplies were halted were: Leukeran 2 mg (chlorambucil); Alkeran 50 mg / 10 mg powder and solvent (melphalan); Alkeran 2 mg (melphalan); Purinethol 50 mg (mercaptopurine); and Thioguanine 40 mg (thioguanine). The price-gouging episode began after Aspen purchased the drugs from GlaxoSmithKline. It then began negotiations with the Italian Medicines Agency over pricing for the cancer medicines. According to the Italian Competition Authority, Aspen also used the threat of a shortage to achieve the high prices it had sought, because the drugs temporarily disappeared from the market. Last month, as part of its continued drive to purchase a portfolio of products from major pharmaceutical companies, AstraZeneca announced that Aspen Global Incorporated (AGI) will acquire the residual rights to the established anesthetic medicines comprising Diprivan, EMLA, Marcaine, Naropin, Carbocaine, Xylocaine/Xylocard/Xyloproct, and Citanest. AstraZeneca had entered into an agreement with AGI in June 2016, under which AGI had gained exclusive commercialization rights to these medicines in markets outside the US. Under the terms of the new agreement, AGI will now acquire the remaining rights to the intellectual property and manufacturing know-how related to the anesthetic medicines for an upfront consideration of US$ 555 million. Additionally, AGI will pay AstraZeneca up to US$ 211 million in performance-related milestones based on sales and gross margin during the period September 1, 2017 to November 30, 2019. Click here to view the major deals in September 2017 (Excel version available) for FREE!   Major CDMOs continue to expand manufacturing footprint Contract development and manufacturing organizations (CDMO) continued to bulk up their manufacturing capabilities. First, Catalent announced it would purchase Cook Pharmica in a transaction valued at US$ 950 million. Catalent intends to use the acquisition to invest aggressively in Cook Pharmica and create a biologics development and manufacturing center of excellence. Another CDMO — Avara Pharmaceutical Services — had acquired a Pfizer facility in Italy in August. Last month, Avara entered into an agreement with GSK to acquire a GSK  consumer healthcare manufacturing facility in Aiken, South Carolina. The terms of the agreement were not disclosed.   Our view Our technology of the month for August 2017 — CAR-T therapy for cancer — got another boost as Gilead (which had acquired Kite Pharma for US$ 11.9 billion in August) received approval last week for Kite’s most advanced CAR-T therapy candidate — axicabtagene ciloleucel (axe-cel). Gilead has announced a price significantly lower than the launch price at which Novartis is selling its CAR-T treatment (Kymriah). While the man who led CAR-T therapy program at Novartis — Vasant Narasimhan — went on to become the Swiss drugmaker’s CEO last month, its ex-CEO Joe Jimenez told Forbes magazine in an interview that he is “ready to return to Silicon Valley.” In his interview, Jimenez, 57, indicated what he thought he could be doing next. “When I think of what really excites me, it’s where biology comes together with technology, like when you think about what’s happening right now in the Valley in California,” Jimenez said. According to the interview, Jimenez is not ruling out joining another big company. He is fascinated by more entrepreneurial startups, and “sees an opportunity for those who understand healthcare to bridge the gap between brilliant techies and a broken system”. He got a glimpse of this potential, he says, from Novartis’ efforts with Verily, the life sciences arm of Alphabet (formerly Google). The companies have been working on smart ocular devices, a contact lens that can monitor the sugar levels of diabetics through their tears. Jimenez says there is a prototype of this lens, which showed him that engineering could benefit from healthcare knowhow. Jimenez isn’t alone in banking on biotech. In September, two former GSK executives — its former CEO Andrew Witty and its one-time research head Moncef Slaoui — announced their moves into the biotech, venture capital space. Our view is that large pools of capital combined with the finest talent would certainly lead to some breakthrough technologies in the pharmaceutical industry in the near future. Watch this space for more. Click here to view the major deals in September 2017 (Excel version available) for FREE    

Impressions: 2659

https://www.pharmacompass.com/radio-compass-blog/pharma-deals-investments-and-m-as-in-september-2017

#PharmaFlow by PHARMACOMPASS
23 Oct 2017

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