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0701472ZG0

0701472ZG0

Synopsis, Chemistry

APIs // Active Pharmaceutical Ingredients

2 API Suppliers, 1 USDMF, 3 NDC API, 1 Listed Suppliers

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2 Drug(s) in Development

2 Drug(s) in Development

DOSSIERs // Finished Dosage Formulations

4 Dossiers, 2 FDA Orange Book, 2 Europe

DRUG PRODUCT COMPOSITION

POWDER;INTRAVENOUS - EQ 250MG BASE/VIAL, POWDER;INTRAVENOUS - EQ 750MG BASE/VIAL

POWDER;INTRAVENOUS - EQ 250MG BASE/VIAL
POWDER;INTRAVENOUS - EQ 750MG BASE/VIAL

RELATED EXCIPIENT COMPANIES

Suppliers, 12 SPI Pharma, 7 Roquette, 3 Gangwal Healthcare, 2 Kerry, 2 Microlex e.U, 2 Gangwal Chemicals, 1 Shijiazhuang Huaxu Pharmaceutical, 1 Rochem International Inc, 1 Sigachi Industries, 1 Shanghai Shenmei Pharmaceutical Technology Co., Ltd, 1 Ingredion Pharma Solutions, 1 DKSH, 1 Pfanstiehl, 1 BASF

EXCIPIENTS BY APPLICATIONS

18 Fillers, Diluents & Binders, 12 Taste Masking, 10 Direct Compression, 10 Chewable & Orodispersible Aids, 5 Parenteral, 4 Thickeners and Stabilizers, 4 Co-Processed Excipients, 3 Solubilizers, 3 Granulation, 3 Disintegrants & Superdisintegrants, 1 API Stability Enhancers

GLOBAL SALES INFORMATION

8 US Medicaid Prescriptions

8 US Medicaid Prescriptions

MARKET PLACE

4 APIs

4 APIs

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2 US Patents, 5 Health Canada Patents

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1 News

1 News

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USA (Orange Book)

Europe

Canada

Australia

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U.S. Medicaid

5.00

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Also known as: Vibativ, Telavancin hcl, 560130-42-9, Td-6424, Td 6424, Telavancin hydrochloride [usan]

Molecular Formula

C₈₀H₁₀₇Cl₃N₁₁O₂₇P

Molecular Weight

1792.1 g/mol

InChI Key

GSSIWSIRBWAZHG-ACOPVEIWSA-N

FDA UNII

0701472ZG0

Telavancin Hydrochloride is the hydrochloride salt form of telavancin, a lipoglycopeptide and a semisynthetic derivative of vancomycin with antibacterial activity against gram-positive bacteria. Like vancomycin, telavancin binds tightly to the D-alanyl-D-alanine residue of cell wall precursors, thereby interfering with bacterial cell wall synthesis. In addition, the lipophilic moiety of telavancin may interact with the lipid bilayer in the bacterial cell membrane, thereby compromising the integrity of cell membrane and causing cell membrane depolarization. This novel mechanism of action may contribute to telavancin's rapid bactericidal activity and its improved activity over vancomycin against some antibiotic resistance gram-positive bacteria.

1 2D Structure

0701472ZG0

2 Identification

2.1 Computed Descriptors

2.1.1 IUPAC Name

(1S,2R,18R,19R,22S,25R,28R,40S)-22-(2-amino-2-oxoethyl)-5,15-dichloro-48-[(2S,3R,4S,5S,6R)-3-[(2S,4S,5S,6S)-4-[2-(decylamino)ethylamino]-5-hydroxy-4,6-dimethyloxan-2-yl]oxy-4,5-dihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy-2,18,32,35,37-pentahydroxy-19-[[(2R)-4-methyl-2-(methylamino)pentanoyl]amino]-20,23,26,42,44-pentaoxo-36-[(phosphonomethylamino)methyl]-7,13-dioxa-21,24,27,41,43-pentazaoctacyclo[26.14.2.23,6.214,17.18,12.129,33.010,25.034,39]pentaconta-3,5,8(48),9,11,14,16,29(45),30,32,34,36,38,46,49-pentadecaene-40-carboxylic acid;hydrochloride

2.1.2 InChI

InChI=1S/C80H106Cl2N11O27P.ClH/c1-7-8-9-10-11-12-13-14-21-85-22-23-87-80(5)32-57(115-37(4)71(80)103)119-70-68(102)67(101)55(34-94)118-79(70)120-69-53-28-41-29-54(69)117-52-20-17-40(27-46(52)82)65(99)63-77(109)91-61(78(110)111)43-30-50(96)44(33-86-35-121(112,113)114)66(100)58(43)42-25-38(15-18-49(42)95)59(74(106)93-63)90-75(107)60(41)89-73(105)48(31-56(83)97)88-76(108)62(92-72(104)47(84-6)24-36(2)3)64(98)39-16-19-51(116-53)45(81)26-39;/h15-20,25-30,36-37,47-48,55,57,59-65,67-68,70-71,79,84-87,94-96,98-103H,7-14,21-24,31-35H2,1-6H3,(H2,83,97)(H,88,108)(H,89,105)(H,90,107)(H,91,109)(H,92,104)(H,93,106)(H,110,111)(H2,112,113,114);1H/t37-,47+,48-,55+,57-,59+,60+,61-,62+,63-,64+,65+,67+,68-,70+,71+,79-,80-;/m0./s1

2.1.3 InChI Key

GSSIWSIRBWAZHG-ACOPVEIWSA-N

2.1.4 Canonical SMILES

CCCCCCCCCCNCCNC1(CC(OC(C1O)C)OC2C(C(C(OC2OC3=C4C=C5C=C3OC6=C(C=C(C=C6)C(C(C(=O)NC(C(=O)NC5C(=O)NC7C8=CC(=C(C=C8)O)C9=C(C(=C(C=C9C(NC(=O)C(C(C1=CC(=C(O4)C=C1)Cl)O)NC7=O)C(=O)O)O)CNCP(=O)(O)O)O)CC(=O)N)NC(=O)C(CC(C)C)NC)O)Cl)CO)O)O)C.Cl

2.1.5 Isomeric SMILES

CCCCCCCCCCNCCN[C@]1(C[C@@H](O[C@H]([C@H]1O)C)O[C@@H]2[C@H]([C@@H]([C@H](O[C@H]2OC3=C4C=C5C=C3OC6=C(C=C(C=C6)[C@H]([C@H](C(=O)N[C@H](C(=O)N[C@H]5C(=O)N[C@@H]7C8=CC(=C(C=C8)O)C9=C(C(=C(C=C9[C@H](NC(=O)[C@H]([C@@H](C1=CC(=C(O4)C=C1)Cl)O)NC7=O)C(=O)O)O)CNCP(=O)(O)O)O)CC(=O)N)NC(=O)[C@@H](CC(C)C)NC)O)Cl)CO)O)O)C.Cl

2.2 Other Identifiers

2.2.1 UNII

0701472ZG0

2.3 Synonyms

2.3.1 MeSH Synonyms

1. Td 6424

2. Td-6424

3. Td6424

4. Telavancin

5. Vibativ

2.3.2 Depositor-Supplied Synonyms

1. Vibativ

2. Telavancin Hcl

3. 560130-42-9

4. Td-6424

5. Td 6424

6. Telavancin Hydrochloride [usan]

7. Televancin Hydrochloride

8. 0701472zg0

9. Telavancin Hydrochloride (usan)

10. Unii-0701472zg0

11. Vibativ (tn)

12. Chembl3301680

13. Chebi:71226

14. Telavancin Hydrochloride [mi]

15. Telavancin Hydrochloride [mart.]

16. Telavancin Hydrochloride [vandf]

17. Televancin Hydrochloride [vandf]

18. Telavancin Hydrochloride [who-dd]

19. Telavancin Hydrochloride [orange Book]

20. D06057

21. Q47495786

22. 380636-75-9

23. Vancomycin, N(sup 3'')-(2-(decylamino)ethyl)-29-(((phosphonomethyl)amino)methyl)-, Monohydrochloride

24. Vancomycin, N3'-(2-(decylamino)ethyl)-29-(((phosphonomethyl)amino)methyl)-, Monohydrochloride

2.4 Create Date

2006-10-25

3 Chemical and Physical Properties

Molecular Formula	C₈₀H₁₀₇Cl₃N₁₁O₂₇P
Molecular Weight	1792.1 g/mol
Hydrogen Bond Donor Count	24
Hydrogen Bond Acceptor Count	31
Rotatable Bond Count	30
Exact Mass	1789.614107 g/mol
Monoisotopic Mass	1789.614107 g/mol
Topological Polar Surface Area	598 Å²
Heavy Atom Count	122
Formal Charge	0
Complexity	3490
Isotope Atom Count	0
Defined Atom Stereocenter Count	18
Undefined Atom Stereocenter Count	0
Defined Bond Stereocenter Count	0
Undefined Bond Stereocenter Count	0
Covalently Bonded Unit Count	2

4 Drug and Medication Information

4.1 Drug Information

1 of 2
Drug Name	Vibativ
PubMed Health	Telavancin (Injection)
Drug Classes	Antibiotic
Drug Label	VIBATIV contains telavancin hydrochloride, a lipoglycopeptide antibacterial that is a synthetic derivative of vancomycin. The chemical name of telavancin hydrochloride is vancomycin,N3''-[2-(decylamino)ethyl]-29-[[(phosphono-methyl)-amino]-methy
Active Ingredient	Telavancin hydrochloride; Telavancin
Dosage Form	Powder; Injectable
Route	injection; Iv (infusion)
Strength	eq 750mg base/vial; 250mg; 750mg; eq 250mg base/vial
Market Status	Prescription
Company	Theravance; Theravance Biopharma

2 of 2
Drug Name	Vibativ
PubMed Health	Telavancin (Injection)
Drug Classes	Antibiotic
Drug Label	VIBATIV contains telavancin hydrochloride, a lipoglycopeptide antibacterial that is a synthetic derivative of vancomycin. The chemical name of telavancin hydrochloride is vancomycin,N3''-[2-(decylamino)ethyl]-29-[[(phosphono-methyl)-amino]-methy
Active Ingredient	Telavancin hydrochloride; Telavancin
Dosage Form	Powder; Injectable
Route	injection; Iv (infusion)
Strength	eq 750mg base/vial; 250mg; 750mg; eq 250mg base/vial
Market Status	Prescription
Company	Theravance; Theravance Biopharma

4.2 Drug Indication

Vibativ is indicated for the treatment of adults with nosocomial pneumonia including ventilator-associated pneumonia, known or suspected to be caused by methicillin-resistant Staphylococcus aureus (MRSA).

Vibativ should be used only in situations where it is known or suspected that other alternatives are not suitable.

Consideration should be given to official guidance on the appropriate use of antibacterial agents.

5 Pharmacology and Biochemistry

5.1 MeSH Pharmacological Classification

Anti-Bacterial Agents

Substances that inhibit the growth or reproduction of BACTERIA. (See all compounds classified as Anti-Bacterial Agents.)

5.2 FDA Pharmacological Classification

5.2.1 Pharmacological Classes

Lipoglycopeptides [EXT]; Lipoglycopeptide Antibacterial [EPC]

5.3 ATC Code

J01XA03