Find Pimozide manufacturers, exporters & distributors on PharmaCompass

NCGC00024888-01

NCGC00024888-01

Synopsis, Chemistry

APIs // Active Pharmaceutical Ingredients

8 API Suppliers, 6 USDMF, 3 CEP/COS, 3 EU WC, 2 NDC API, 2 Listed Suppliers

DEVELOPMENTS

1 Drug(s) in Development

1 Drug(s) in Development

PRICE INFORMATION

API Reference Price, API Exports, API Imports

INTERMEDIATES

4 Suppliers

4 Suppliers

DOSSIERs // Finished Dosage Formulations

13 Dossiers, 4 FDA Orange Book, 1 Europe, 4 Canada, 2 South Africa, 2 Listed Dossiers

DRUG PRODUCT COMPOSITION

TABLET;ORAL - 1MG **Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons**, TABLET;ORAL - 2MG **Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons**

TABLET;ORAL - 1MG **Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons**
TABLET;ORAL - 2MG **Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons**

RELATED EXCIPIENT COMPANIES

Suppliers, 13 Roquette, 10 Kerry, 8 Sigachi Industries, 6 Gangwal Healthcare, 5 Microlex e.U, 4 SPI Pharma, 3 DFE Pharma, 3 Shanghai Shenmei Pharmaceutical Technology Co., Ltd, 3 Gangwal Chemicals, 2 Vasa Pharmachem, 2 Anhui Sunhere Pharmaceutical Excipients Co.,Ltd, 2 Ingredion Pharma Solutions, 1 Ideal Cures Pvt Ltd, 1 Prachin Chemical, 1 Seppic, 1 Pharmatrans-Sanaq

EXCIPIENTS BY APPLICATIONS

29 Fillers, Diluents & Binders, 17 Direct Compression, 9 Thickeners and Stabilizers, 9 Disintegrants & Superdisintegrants, 9 Co-Processed Excipients, 7 Granulation, 6 Lubricants & Glidants, 5 Controlled & Modified Release, 5 Chewable & Orodispersible Aids, 5 Taste Masking, 3 Coating Systems & Additives, 1 Film Formers & Plasticizers, 1 Rheology Modifiers

GLOBAL SALES INFORMATION

13 US Medicaid Prescriptions, 3 Finished Drug Prices

MARKET PLACE

1 APIs

1 APIs

ANALYTICAL SOLUTION(s)

3 EDQM Standards, 1 USP Standards, 1 Other Ref. Standards

DIGITAL CONTENT

2 News

2 News

Product Search

API SUPPLIERS

API Suppliers

US DMFs Filed

CEP/COS Certifications

JDMFs Filed

Other Certificates

Other Suppliers

API REF. PRICE (USD / KG)

7,849

API Market Place

INTERMEDIATES

DOSSIERS // FDF

USA (Orange Book)

Europe

Canada

Australia

South Africa

Uploaded Dossiers

GLOBAL SALES (USD Million)

U.S. Medicaid

14.00

Annual Reports

FDF Market Place

EXCIPIENTS

PATENTS & EXCLUSIVITIES

USFDA Orange Book Patents

USFDA Exclusivities

DIGITAL CONTENT

Blog #PharmaFlow

News

REF STANDARD

EDQM

USP

Other Listed Suppliers

SERVICES

Also known as: 2062-78-4, Orap, Opiran, Pimozidum, Mcn-jr-6238, Pimozidum [inn-latin]

Molecular Formula

C₂₈H₂₉F₂N₃O

Molecular Weight

461.5 g/mol

InChI Key

YVUQSNJEYSNKRX-UHFFFAOYSA-N

FDA UNII

1HIZ4DL86F

A diphenylbutylpiperidine that is effective as an antipsychotic agent and as an alternative to HALOPERIDOL for the suppression of vocal and motor tics in patients with Tourette syndrome. Although the precise mechanism of action is unknown, blockade of postsynaptic dopamine receptors has been postulated. (From AMA Drug Evaluations Annual, 1994, p403)

Pimozide is a Typical Antipsychotic.

1 2D Structure

NCGC00024888-01

2 Identification

2.1 Computed Descriptors

2.1.1 IUPAC Name

3-[1-[4,4-bis(4-fluorophenyl)butyl]piperidin-4-yl]-1H-benzimidazol-2-one

2.1.2 InChI

InChI=1S/C28H29F2N3O/c29-22-11-7-20(8-12-22)25(21-9-13-23(30)14-10-21)4-3-17-32-18-15-24(16-19-32)33-27-6-2-1-5-26(27)31-28(33)34/h1-2,5-14,24-25H,3-4,15-19H2,(H,31,34)

2.1.3 InChI Key

YVUQSNJEYSNKRX-UHFFFAOYSA-N

2.1.4 Canonical SMILES

C1CN(CCC1N2C3=CC=CC=C3NC2=O)CCCC(C4=CC=C(C=C4)F)C5=CC=C(C=C5)F

2.2 Other Identifiers

2.2.1 UNII

1HIZ4DL86F

2.3 Synonyms

2.3.1 MeSH Synonyms

1. Antalon

2. Orap

3. Orap Forte

4. R-6238

5. R6238

2.3.2 Depositor-Supplied Synonyms

1. 2062-78-4

2. Orap

3. Opiran

4. Pimozidum

5. Mcn-jr-6238

6. Pimozidum [inn-latin]

7. R-6238

8. R 6238

9. R6238

10. Nsc 170984

11. Mcn-jr 6238

12. 3-[1-[4,4-bis(4-fluorophenyl)butyl]piperidin-4-yl]-1h-benzimidazol-2-one

13. 1-[1-[4,4-bis(4-fluorophenyl)butyl]-4-piperidinyl]-1,3-dihydro-2h-benzimidazol-2-one

14. 2h-benzimidazol-2-one, 1-[1-[4,4-bis(4-fluorophenyl)butyl]-4-piperidinyl]-1,3-dihydro-

15. Nsc-170984

16. 1-(1-(4,4-bis(p-fluorophenyl)butyl)-4-piperidyl)-2-benzimidazolinone

17. 1-[1-[4,4-bis(p-fluorophenyl)butyl]-4-piperidyl]-2-benzimidazolinone

18. 1hiz4dl86f

19. Chembl1423

20. 1-(4,4-bis(p-fluorophenyl)butyl)-4-(2-oxo-1-benzimidazolinyl)piperidine

21. Mls000028410

22. Mls002702058

23. Chebi:8212

24. Nsc170984

25. 1-{1-[4,4-bis(4-fluorophenyl)butyl]piperidin-4-yl}-1,3-dihydro-2h-benzimidazol-2-one

26. 1-{1-[4,4-bis(4-fluorophenyl)butyl]piperidin-4-yl}-2,3-dihydro-1h-1,3-benzodiazol-2-one

27. 2h-benzimidazol-2-one, 1-(1-(4,4-bis(4-fluorophenyl)butyl)-4-piperidinyl)-1,3-dihydro-

28. Pimozida

29. Ncgc00015802-08

30. Ncgc00015802-18

31. Primozida

32. Smr000058385

33. Cas-2062-78-4

34. R 623

35. R-623

36. Dsstox_cid_3474

37. 1-(1-(4,4-bis(4-fluorophenyl)butyl)piperidin-4-yl)-1h-benzo[d]imidazol-2(3h)-one

38. Dsstox_rid_77042

39. Dsstox_gsid_23474

40. Primozida [inn-spanish]

41. Primozide

42. Pimozida [inn-spanish]

43. 1-[4,4-bis(p-fluorophenyl)butyl]-4-(2-oxo-1-benzimidazolinyl)piperidine

44. Ccris 9172

45. Orap (tn)

46. Sr-01000075392

47. Einecs 218-171-7

48. Unii-1hiz4dl86f

49. Brn 0729089

50. 1-(1-(4,4-bis(4-fluorophenyl)butyl)-4-piperidinyl)-1,3-dihydro-2h-benzimidazol-2-one

51. Prestwick_395

52. Mfcd00055081

53. Pimozide [usan:usp:inn:ban:jan]

54. Spectrum_000445

55. Tocris-0937

56. Pimozide [usan]

57. Pimozide [inn]

58. Pimozide [jan]

59. Pimozide [mi]

60. Pimozide [vandf]

61. Opera_id_1580

62. Prestwick0_000308

63. Prestwick1_000308

64. Prestwick2_000308

65. Prestwick3_000308

66. Spectrum2_001026

67. Spectrum3_001451

68. Spectrum4_000420

69. Spectrum5_001308

70. Lopac-p-1793

71. Pimozide [mart.]

72. Gtpl90

73. Pimozide [usp-rs]

74. Pimozide [who-dd]

75. Ncimech_000356

76. P 1793

77. Lopac0_000946

78. Schembl41584

79. Bspbio_000276

80. Bspbio_001439

81. Bspbio_002941

82. Kbiogr_000720

83. Kbioss_000925

84. 5-24-02-00367 (beilstein Handbook Reference)

85. Mls001077311

86. Bidd:gt0435

87. Divk1c_000386

88. Methyl-(2-m-tolylethyl)amine

89. Spectrum1501134

90. Pimozide (jp17/usp/inn)

91. Spbio_001211

92. Spbio_002495

93. Pimozide [orange Book]

94. Bpbio1_000304

95. Schembl7519553

96. Pimozide [ep Monograph]

97. Dtxsid8023474

98. Pimozide [usp Monograph]

99. Bcbcmap01_000043

100. Hms501d08

101. Kbio1_000386

102. Kbio2_000925

103. Kbio2_003493

104. Kbio2_006061

105. Kbio3_002441

106. Ninds_000386

107. Hms1568n18

108. Hms1791h21

109. Hms1921h19

110. Hms1989h21

111. Hms2089c11

112. Hms2092f09

113. Hms2095n18

114. Hms2231p23

115. Hms3262n14

116. Hms3267e19

117. Hms3370n13

118. Hms3402h21

119. Hms3411j16

120. Hms3675j16

121. Hms3712n18

122. Pharmakon1600-01501134

123. Zinc4175630

124. Tox21_110224

125. Tox21_301586

126. Tox21_500946

127. Bdbm50334150

128. Ccg-35918

129. Ccg-36461

130. Ccg-39728

131. Nsc757854

132. S4358

133. 2-benzimidazolinone, 1-[1-[4,4-bis(p-fluorophenyl)butyl]-4-piperidyl]-

134. 3-[1-[4,4-bis(4-fluorophenyl)butyl]-4-piperidyl]-1h-benzimidazol-2-one

135. Akos024458706

136. Tox21_110224_1

137. Db01100

138. Lp00946

139. Nsc-757854

140. Sdccgsbi-0050920.p004

141. Idi1_000386

142. Smp1_000241

143. Ncgc00015802-01

144. Ncgc00015802-02

145. Ncgc00015802-03

146. Ncgc00015802-04

147. Ncgc00015802-05

148. Ncgc00015802-06

149. Ncgc00015802-07

150. Ncgc00015802-09

151. Ncgc00015802-10

152. Ncgc00015802-11

153. Ncgc00015802-12

154. Ncgc00015802-13

155. Ncgc00015802-14

156. Ncgc00015802-15

157. Ncgc00015802-16

158. Ncgc00015802-26

159. Ncgc00015802-29

160. Ncgc00016601-01

161. Ncgc00022282-03

162. Ncgc00024888-01

163. Ncgc00024888-02

164. Ncgc00024888-03

165. Ncgc00024888-04

166. Ncgc00024888-05

167. Ncgc00024888-06

168. Ncgc00024888-07

169. Ncgc00255294-01

170. Ncgc00261631-01

171. As-13916

172. Hy-12987

173. Sbi-0050920.p003

174. Ab00052215

175. Cs-0012921

176. Eu-0100946

177. Ft-0673903

178. Sw196639-3

179. C07566

180. D00560

181. F70142

182. Ab00052215-06

183. Ab00052215_07

184. Ab00052215_08

185. 062p784

186. L000494

187. Q144085

188. Wln: T56 Bmvnj D- Dt6ntj A3yr Df&r Df

189. J-013477

190. Sr-01000075392-1

191. Sr-01000075392-3

192. Sr-01000075392-4

193. Sr-01000075392-6

194. Brd-k01292756-001-06-0

195. Brd-k01292756-001-13-6

196. Pimozide, European Pharmacopoeia (ep) Reference Standard

197. Z241910386

198. 2-benzimidazolinone,4-bis(p-fluorophenyl)butyl]-4-piperidyl]-

199. N-benzyl-n-(3-isobutoxy-2-(pyrrolidin-1-yl)propyl)benzenamine

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

201. 1-[1-[4,4-bis(p-flurophenyl)butyl]-4-piperidyl]-2-benzimidazolinone

202. 1-(1-(4,4-bis(4-fluorophenyl)butyl)-4-piperidyl)-2-benzimidazolinone

203. 1-(1-(4,4-bis(4-fluorophenyl)butyl)piperidin-4-yl)-1,3-dihydro-2h-benzo[d]imidazol-2-one

204. 1-{1-[4,4-bis-(4-fluoro-phenyl)-butyl]-piperidin-4-yl}-1,3-dihydro-benzoimidazol-2-one

205. 2h-benzimidazol-2-one,4-bis(4-fluorophenyl)butyl]-4-piperidinyl]-1,3-dihydro-

206. 1-{1-[4,4-bis-(4-fluoro-phenyl)-butyl]-piperidin-4-yl}-1,3-dihydro-benzoimidazol-2-one(pimozide)

207. 2h-benzimidazol-2-one, 1-(1-(4,4-bis(4-fluorophenyl)butyl)-4-piperidinyl)-1,3-dihydro

208. Pimozide (1-[1-[4,4-bis(4-fluorophenyl)butyl]-4-piperidinyl]-1,3-dihydro-2h-benzimidaol-2-one)

209. Pimozide1-{1-[4,4-bis-(4-fluoro-phenyl)-butyl]-piperidin-4-yl}-1,3-dihydro-benzoimidazol-2-one

2.4 Create Date

2005-03-26

3 Chemical and Physical Properties

Molecular Formula	C₂₈H₂₉F₂N₃O
Molecular Weight	461.5 g/mol
XLogP3	6.3
Hydrogen Bond Donor Count	1
Hydrogen Bond Acceptor Count	4
Rotatable Bond Count	7
Exact Mass	461.22786888 g/mol
Monoisotopic Mass	461.22786888 g/mol
Topological Polar Surface Area	35.6 Å²
Heavy Atom Count	34
Formal Charge	0
Complexity	632
Isotope Atom Count	0
Defined Atom Stereocenter Count	0
Undefined Atom Stereocenter Count	0
Defined Bond Stereocenter Count	0
Undefined Bond Stereocenter Count	0
Covalently Bonded Unit Count	1

4 Drug and Medication Information

4.1 Drug Information

1 of 2
Drug Name	Orap
PubMed Health	Pimozide (By mouth)
Drug Classes	Antipsychotic
Drug Label	ORAP (pimozide) is an orally active antipsychotic agent of the diphenyl-butylpiperidine series. The structural formula of pimozide, 1-[1-[4,4-bis(4-fluorophenyl)butyl]-4-piperidinyl]-1,3-dihydro-2H-benzimidazole-2-one is:The solubility of pimozide...
Active Ingredient	Pimozide
Dosage Form	Tablet
Route	Oral
Strength	1mg; 2mg
Market Status	Prescription
Company	Teva

2 of 2
Drug Name	Orap
PubMed Health	Pimozide (By mouth)
Drug Classes	Antipsychotic
Drug Label	ORAP (pimozide) is an orally active antipsychotic agent of the diphenyl-butylpiperidine series. The structural formula of pimozide, 1-[1-[4,4-bis(4-fluorophenyl)butyl]-4-piperidinyl]-1,3-dihydro-2H-benzimidazole-2-one is:The solubility of pimozide...
Active Ingredient	Pimozide
Dosage Form	Tablet
Route	Oral
Strength	1mg; 2mg
Market Status	Prescription
Company	Teva

4.2 Drug Indication

Used for the suppression of motor and phonic tics in patients with Tourette's Disorder who have failed to respond satisfactorily to standard treatment.

5 Pharmacology and Biochemistry

5.1 Pharmacology

Pimozide is an orally active antipsychotic drug product which shares with other antipsychotics the ability to blockade dopaminergic receptors on neurons in the central nervous system. However, receptor blockade is often accompanied by a series of secondary alterations in central dopamine metabolism and function which may contribute to both pimozide's therapeutic and untoward effects. In addition, pimozide, in common with other antipsychotic drugs, has various effects on other central nervous system receptor systems which are not fully characterized. Pimozide also has less potential for inducing sedation and hypotension as it has more specific dopamine receptor blocking activity than other neuroleptic agents (and is therefore a suitable alternative to haloperidol).

5.2 MeSH Pharmacological Classification

Dopamine Antagonists

Drugs that bind to but do not activate DOPAMINE RECEPTORS, thereby blocking the actions of dopamine or exogenous agonists. Many drugs used in the treatment of psychotic disorders (ANTIPSYCHOTIC AGENTS) are dopamine antagonists, although their therapeutic effects may be due to long-term adjustments of the brain rather than to the acute effects of blocking dopamine receptors. Dopamine antagonists have been used for several other clinical purposes including as ANTIEMETICS, in the treatment of Tourette syndrome, and for hiccup. Dopamine receptor blockade is associated with NEUROLEPTIC MALIGNANT SYNDROME. (See all compounds classified as Dopamine Antagonists.)

Antipsychotic Agents

Agents that control agitated psychotic behavior, alleviate acute psychotic states, reduce psychotic symptoms, and exert a quieting effect. They are used in SCHIZOPHRENIA; senile dementia; transient psychosis following surgery; or MYOCARDIAL INFARCTION; etc. These drugs are often referred to as neuroleptics alluding to the tendency to produce neurological side effects, but not all antipsychotics are likely to produce such effects. Many of these drugs may also be effective against nausea, emesis, and pruritus. (See all compounds classified as Antipsychotic Agents.)

Anti-Dyskinesia Agents

Drugs used in the treatment of movement disorders. Most of these act centrally on dopaminergic or cholinergic systems. Among the most important clinically are those used for the treatment of Parkinson disease (ANTIPARKINSON AGENTS) and those for the tardive dyskinesias. (See all compounds classified as Anti-Dyskinesia Agents.)

5.3 FDA Pharmacological Classification

5.3.1 Active Moiety

PIMOZIDE

5.3.2 FDA UNII

1HIZ4DL86F

5.3.3 Pharmacological Classes

Typical Antipsychotic [EPC]

5.4 ATC Code

N05AG02

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

N05 - Psycholeptics

N05A - Antipsychotics

N05AG - Diphenylbutylpiperidine derivatives

N05AG02 - Pimozide

5.5 Absorption, Distribution and Excretion

Absorption

Greater than 50% absorption after oral administration. Serum peak appears 6-8 hours post ingestion.

5.6 Metabolism/Metabolites

Notable first-pass metabolism in the liver, primarily by N-dealkylation via the cytochrome P450 isoenzymes CYP3A and CYP1A2 (and possibly CYP2D6). The activity of the two major metabolites has not been determined.

Pimozide has known human metabolites that include 1,3- dihydro-1-(4-piperidinyl)-2H-benzimidazol-2-one (DHPBI).

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

5.7 Biological Half-Life

29 ± 10 hours (single-dose study of healthy volunteers).

5.8 Mechanism of Action

The ability of pimozide to suppress motor and phonic tics in Tourette's Disorder is thought to be primarily a function of its dopaminergic blocking activity. Pimozide binds and inhibits the dopamine D2 receptor in the CNS.

Market Place

Home

Post Enquiry

Market Place