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Synopsis

ACTIVE PHARMA INGREDIENTS

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Chemistry

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Also known as: Gs-6207, 2189684-44-2, Gs-hiv, Gs-ca2, Gs-ca-2, Lenacapavir [usan]
Molecular Formula
C39H32ClF10N7O5S2
Molecular Weight
968.3  g/mol
InChI Key
BRYXUCLEHAUSDY-WEWMWRJBSA-N
FDA UNII
A9A0O6FB4H

Lenacapavir
Lenacapavir is under investigation in clinical trial NCT04150068 (Study to Evaluate the Safety and Efficacy of Lenacapavir in Combination With an Optimized Background Regimen in Heavily Treatment Experienced Participants Living With HIV-1 Infection With Multidrug Resistance).
1 2D Structure

Lenacapavir

2 Identification
2.1 Computed Descriptors
2.1.1 IUPAC Name
N-[(1S)-1-[3-[4-chloro-3-(methanesulfonamido)-1-(2,2,2-trifluoroethyl)indazol-7-yl]-6-(3-methyl-3-methylsulfonylbut-1-ynyl)pyridin-2-yl]-2-(3,5-difluorophenyl)ethyl]-2-[(2S,4R)-5,5-difluoro-9-(trifluoromethyl)-7,8-diazatricyclo[4.3.0.02,4]nona-1(6),8-dien-7-yl]acetamide
2.1.2 InChI
InChI=1S/C39H32ClF10N7O5S2/c1-36(2,63(3,59)60)10-9-21-5-6-22(23-7-8-26(40)30-32(23)57(17-37(43,44)45)54-35(30)55-64(4,61)62)31(51-21)27(13-18-11-19(41)14-20(42)12-18)52-28(58)16-56-34-29(33(53-56)39(48,49)50)24-15-25(24)38(34,46)47/h5-8,11-12,14,24-25,27H,13,15-17H2,1-4H3,(H,52,58)(H,54,55)/t24-,25+,27-/m0/s1
2.1.3 InChI Key
BRYXUCLEHAUSDY-WEWMWRJBSA-N
2.1.4 Canonical SMILES
CC(C)(C#CC1=NC(=C(C=C1)C2=C3C(=C(C=C2)Cl)C(=NN3CC(F)(F)F)NS(=O)(=O)C)C(CC4=CC(=CC(=C4)F)F)NC(=O)CN5C6=C(C7CC7C6(F)F)C(=N5)C(F)(F)F)S(=O)(=O)C
2.1.5 Isomeric SMILES
CC(C)(C#CC1=NC(=C(C=C1)C2=C3C(=C(C=C2)Cl)C(=NN3CC(F)(F)F)NS(=O)(=O)C)[C@H](CC4=CC(=CC(=C4)F)F)NC(=O)CN5C6=C([C@H]7C[C@H]7C6(F)F)C(=N5)C(F)(F)F)S(=O)(=O)C
2.2 Other Identifiers
2.2.1 UNII
A9A0O6FB4H
2.3 Synonyms
2.3.1 MeSH Synonyms

1. Gs-ca1

2.3.2 Depositor-Supplied Synonyms

1. Gs-6207

2. 2189684-44-2

3. Gs-hiv

4. Gs-ca2

5. Gs-ca-2

6. Lenacapavir [usan]

7. Gs-ca1

8. A9a0o6fb4h

9. Gs-714207

10. Gs6207

11. N-[(1s)-1-[3-[4-chloro-3-(methanesulfonamido)-1-(2,2,2-trifluoroethyl)indazol-7-yl]-6-(3-methyl-3-methylsulfonylbut-1-ynyl)pyridin-2-yl]-2-(3,5-difluorophenyl)ethyl]-2-[(2s,4r)-5,5-difluoro-9-(trifluoromethyl)-7,8-diazatricyclo[4.3.0.02,4]nona-1(6),8-dien-7-yl]acetamide

12. N-((s)-1-(3-(4-chloro-3-(methylsulfonamido)-1-(2,2,2-trifluoroethyl)-1h-indazol-7-yl)-6-(3-methyl-3-(methylsulfonyl)but-1-yn-1-yl)pyridin-2-yl)-2-(3,5-difluorophenyl)ethyl)-2-((3bs,4ar)-5,5-difluoro-3-(trifluoromethyl)-3b,4,4a,5-tetrahydro-1h-cyclopropa[3,4]cyclopenta[1,2-c]pyrazol-1-yl)acetamide

13. N-[(1s)-1-(3-{4-chloro-3-[(methylsulfonyl)amino]-1-(2,2,2-trifluoroethyl)-1h-indazol-7-yl}-6-[3-methyl-3-(methylsulfonyl)but-1-yn-1-yl]pyridin-2-yl)-2-(3,5-difluorophenyl)ethyl]-2-[(3bs,4ar)-5,5-difluoro-3-(trifluoromethyl)-3b,4,4a,5-tetrahydro-1h-cyclopropa[3,4]cyclopenta[1,2-c]pyrazol-1-yl]acetamide

14. Qng

15. Lenacapavir [inn]

16. Unii-a9a0o6fb4h

17. Lenacapavir [who-dd]

18. Chembl4594438

19. Schembl19875642

20. Gtpl11446

21. Ex-a5518

22. Who 11108

23. At20076

24. Hy-111964

25. Cs-0094695

26. 1h-cyclopropa(3,4)cyclopenta(1,2-c)pyrazole, N-((1s)-1-(3-(4-chloro-3-((methylsulfonyl)amino)-1-(2,2,2-trifluoroethyl)-1h-indazol-7-yl)-6-(3-methyl-3-(methylsulfonyl)-1-butyn-1-yl)-2-pyridinyl)-2-(3,5-difluorophenyl)ethyl)-5,5-difluoro-3b,4,4a,5-tetrahydro-3-(trifluoromethyl)-, (3bs,4ar)-

27. N-((1s)-1-(3-(4-chloro-3-(methanesulfonamido)-1-(2,2,2-trifluoroethyl)-1h-indazol-7-yl)-6-(3-(methanesulfonyl)-3-methylbut-1-yn-1-yl)pyridin-2-yl)-2-(3,5- Difluorophenyl)ethyl)-2-((3bs,4ar)-5,5-difluoro-3-(trifluoromethyl)-3b,4,4a,5-tetrahydro-1h-cyclopropa(3,4)cyclopenta(1,2-c)pyrazol-1-yl)acetamide

28. N-[(1s)-1-[3-[4-chloro-3-(methanesulfonamido)-1-(2,2,2-trifluoroethyl)indazol-7-yl]-6-(3-methyl-3-methylsulfonyl-but-1-ynyl)-2-pyridyl]-2-(3,5-difluorophenyl)ethyl]-2-[difluoro(trifluoromethyl)[?]yl]acetamide

2.4 Create Date
2018-05-16
3 Chemical and Physical Properties
Molecular Weight 968.3 g/mol
Molecular Formula C39H32ClF10N7O5S2
XLogP36.4
Hydrogen Bond Donor Count2
Hydrogen Bond Acceptor Count19
Rotatable Bond Count13
Exact Mass967.1435188 g/mol
Monoisotopic Mass967.1435188 g/mol
Topological Polar Surface Area175 Ų
Heavy Atom Count64
Formal Charge0
Complexity2040
Isotope Atom Count0
Defined Atom Stereocenter Count3
Undefined Atom Stereocenter Count0
Defined Bond Stereocenter Count0
Undefined Bond Stereocenter Count0
Covalently Bonded Unit Count1
4 Drug and Medication Information
4.1 Drug Indication

Treatment of human immunodeficiency virus (HIV-1) infection


* Sunlenca injection: , in combination with other antiretroviral(s), is indicated for the treatment of adults with multidrug resistant HIV 1 infection for whom it is otherwise not possible to construct a suppressive anti viral regimen (see sections 4. 2 and 5. 1).

* Sunlenca tablet: , in combination with other antiretroviral(s), is indicated for the treatment of adults with multidrug resistant HIV 1 infection for whom it is otherwise not possible to construct a suppressive anti viral regimen, for oral loading prior to administration of long-acting lenacapavir injection (see sections 4. 2 and 5. 1).


5 Pharmacology and Biochemistry
5.1 ATC Code

J05AX


J - Antiinfectives for systemic use

J05 - Antivirals for systemic use

J05A - Direct acting antivirals

J05AX - Other antivirals

J05AX31 - Lenacapavir


NDC API

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LENACAPAVIR SODIUM

NDC Package Code : 54014-6902

Start Marketing Date : 2022-12-22

End Marketing Date : 2024-12-31

Dosage Form (Strength) : POWDER (1kg/kg)

Marketing Category : BULK INGREDIENT

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Yuhan Chemical Inc

South Korea
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Yuhan Chemical Inc

South Korea
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LENACAPAVIR

NDC Package Code : 66721-830

Start Marketing Date : 2022-08-17

End Marketing Date : 2024-12-31

Dosage Form (Strength) : POWDER (20kg/20kg)

Marketing Category : BULK INGREDIENT

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INTERMEDIATES SUPPLIERS

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01

  • fda
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  • WHO-GMP

Virtual BoothShanghai Minbiotech is the leading producer of biopharmaceuticals and a variety of high-end generic & innovative drugs.

CAS Number : 1620056-83-8

End Use API : Lenacapavir

About The Company : ​Headquartered in Fengxian District, Shanghai Minbiotech Co., Ltd. is a company specializing in the R&D and production of advanced pharmaceutical intermediate...

Shanghai Minbiotech CB

02

  • fda
  • EDQM
  • WHO-GMP

Virtual BoothShanghai Minbiotech is the leading producer of biopharmaceuticals and a variety of high-end generic & innovative drugs.

CAS Number : 2109226-54-0

End Use API : Lenacapavir

About The Company : ​Headquartered in Fengxian District, Shanghai Minbiotech Co., Ltd. is a company specializing in the R&D and production of advanced pharmaceutical intermediate...

Shanghai Minbiotech CB

03

  • fda
  • EDQM
  • WHO-GMP

Virtual BoothShanghai Minbiotech is the leading producer of biopharmaceuticals and a variety of high-end generic & innovative drugs.

CAS Number : 1620056-47-4

End Use API : Lenacapavir

About The Company : ​Headquartered in Fengxian District, Shanghai Minbiotech Co., Ltd. is a company specializing in the R&D and production of advanced pharmaceutical intermediate...

Shanghai Minbiotech CB

04

  • fda
  • EDQM
  • WHO-GMP

Virtual BoothShanghai Minbiotech is the leading producer of biopharmaceuticals and a variety of high-end generic & innovative drugs.

CAS Number : 2189684-54-4

End Use API : Lenacapavir

About The Company : ​Headquartered in Fengxian District, Shanghai Minbiotech Co., Ltd. is a company specializing in the R&D and production of advanced pharmaceutical intermediate...

Shanghai Minbiotech CB

05

  • fda
  • EDQM
  • WHO-GMP

Virtual BoothShanghai Minbiotech is the leading producer of biopharmaceuticals and a variety of high-end generic & innovative drugs.

CAS Number : 2189684-53-3

End Use API : Lenacapavir

About The Company : ​Headquartered in Fengxian District, Shanghai Minbiotech Co., Ltd. is a company specializing in the R&D and production of advanced pharmaceutical intermediate...

Shanghai Minbiotech CB

06

PPS Boston
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  • EDQM
  • WHO-GMP

Virtual BoothPorton Pharma Solutions: Value creation via innovation & discovery through technical platforms.

CAS Number : 1620056-83-8

End Use API : Lenacapavir

About The Company : Porton Pharma Solutions Ltd. was founded in 2005, & the company's stock was successfully listed in Shenzhen Stock Exchange in 2014. Our R&D, manufacturing & ope...

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07

SCI Pharmtech

Taiwan
PPS Boston
Not Confirmed
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  • fda
  • EDQM
  • WHO-GMP

Virtual BoothSCI Pharmtech offers high-quality, cost-effective APIs, advanced intermediates, & custom products with global expertise and precision.

CAS Number : 91-00-9

End Use API : Lenacapavir

About The Company : SCI Pharmtech Inc. offers APIs, advanced intermediates, and custom products, focusing on quick development and cost-effective production. Our research labs, pil...

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SCI Pharmtech

Taiwan
PPS Boston
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  • EDQM
  • WHO-GMP

Virtual BoothSCI Pharmtech offers high-quality, cost-effective APIs, advanced intermediates, & custom products with global expertise and precision.

CAS Number : 91-00-9

End Use API : Lenacapavir

About The Company : SCI Pharmtech Inc. offers APIs, advanced intermediates, and custom products, focusing on quick development and cost-effective production. Our research labs, pil...

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09

PPS Boston
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PPS Boston
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CAS Number : 2189684-53-3

End Use API : Lenacapavir

About The Company : Saptagir Laboratories Private incorporated in 2016, is a manufacturer and supplier of Active Pharmaceutical Ingredients (APIs) and Intermediates for a wide rang...

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PPS Boston
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CAS Number : 2189684-54-4

End Use API : Lenacapavir

About The Company : Saptagir Laboratories Private incorporated in 2016, is a manufacturer and supplier of Active Pharmaceutical Ingredients (APIs) and Intermediates for a wide rang...

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FDF Dossiers

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Compamed
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LENACAPAVIR SODIUM

Brand Name : SUNLENCA

Dosage Form : SOLUTION;SUBCUTANEOUS

Dosage Strength : EQ 463.5MG BASE/1.5ML (EQ 309MG BASE/ML)

Packaging :

Approval Date : 2022-12-22

Application Number : 215973

Regulatory Info : RX

Registration Country : USA

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LENACAPAVIR SODIUM

Brand Name : SUNLENCA

Dosage Form : TABLET;ORAL

Dosage Strength : EQ 300MG BASE

Packaging :

Approval Date : 2022-12-22

Application Number : 215974

Regulatory Info : RX

Registration Country : USA

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FDA Orange Book

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LENACAPAVIR SODIUM

Brand Name : SUNLENCA

Dosage Form : SOLUTION;SUBCUTANEOUS

Dosage Strength : EQ 463.5MG BASE/1.5ML (EQ 309MG BASE/ML)

Approval Date : 2022-12-22

Application Number : 215973

RX/OTC/DISCN : RX

RLD : Yes

TE Code :

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LENACAPAVIR SODIUM

Brand Name : SUNLENCA

Dosage Form : TABLET;ORAL

Dosage Strength : EQ 300MG BASE

Approval Date : 2022-12-22

Application Number : 215974

RX/OTC/DISCN : RX

RLD : Yes

TE Code :

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DATA COMPILATION #PharmaFlow

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STOCK RECAP #PipelineProspector

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NEWS #PharmaBuzz

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https://www.fiercebiotech.com/biotech/merck-gilead-long-acting-oral-combo-suppresses-hiv-48-weeks-setting-stage-pivotal-program

FIERCE BIOTECH
22 Oct 2024

https://www.businesswire.com/news/home/20241006981896/en

BUSINESSWIRE
07 Oct 2024

https://economictimes.indiatimes.com/industry/healthcare/biotech/pharmaceuticals/quick-access-to-key-hiv-drug-hinges-on-waiver-of-local-clinical-trials-experts/articleshow/113916321.cms

ECONOMICTIMES
03 Oct 2024

https://www.drreddys.com/cms/cms/sites/default/files/2024-10/DRL%20Press%20release-%20VL%20with%20Gilead-%20%20final-%20Oct%202nd%2C%202024.pdf

PRESS RELEASE
02 Oct 2024

https://www.fiercepharma.com/pharma/gilead-looks-redefine-hiv-prep-market-2025-long-acting-sunlenca-launch

FIERCE PHARMA
09 Aug 2024

https://www.businesswire.com/news/home/20240724232867/en

BUSINESSWIRE
24 Jul 2024

Patents & EXCLUSIVITIES

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US Patents

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LENACAPAVIR SODIUM

US Patent Number : 9951043

Drug Substance Claim : Y

Drug Product Claim : Y

Application Number : 215973

Patent Use Code : U-3507

Delist Requested :

Patent Use Description :

Patent Expiration Date : 2034-02-28

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LENACAPAVIR SODIUM

US Patent Number : 9951043

Drug Substance Claim : Y

Drug Product Claim : Y

Application Number : 215974

Patent Use Code : U-3507

Delist Requested :

Patent Use Description :

Patent Expiration Date : 2034-02-28

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LENACAPAVIR SODIUM

US Patent Number : 10654827

Drug Substance Claim :

Drug Product Claim :

Application Number : 215974

Patent Use Code : U-3507

Delist Requested :

Patent Use Description :

Patent Expiration Date : 2037-08-17

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04

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LENACAPAVIR SODIUM

US Patent Number : 11267799

Drug Substance Claim : Y

Drug Product Claim :

Application Number : 215974

Patent Use Code :

Delist Requested :

Patent Use Description :

Patent Expiration Date : 2038-08-16

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LENACAPAVIR SODIUM

US Patent Number : 10071985

Drug Substance Claim : Y

Drug Product Claim : Y

Application Number : 215973

Patent Use Code :

Delist Requested :

Patent Use Description :

Patent Expiration Date : 2037-08-17

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LENACAPAVIR SODIUM

US Patent Number : 10071985

Drug Substance Claim : Y

Drug Product Claim : Y

Application Number : 215974

Patent Use Code :

Delist Requested :

Patent Use Description :

Patent Expiration Date : 2037-08-17

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07

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LENACAPAVIR SODIUM

US Patent Number : 11944611

Drug Substance Claim : Y

Drug Product Claim : Y

Application Number : 215974

Patent Use Code : U-3507

Delist Requested :

Patent Use Description :

Patent Expiration Date : 2041-06-04

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08

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LENACAPAVIR SODIUM

US Patent Number : 11267799

Drug Substance Claim : Y

Drug Product Claim :

Application Number : 215973

Patent Use Code :

Delist Requested :

Patent Use Description :

Patent Expiration Date : 2038-08-16

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09

arrow
Compamed
Not Confirmed
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LENACAPAVIR SODIUM

US Patent Number : 11944611

Drug Substance Claim :

Drug Product Claim :

Application Number : 215973

Patent Use Code : U-3507

Delist Requested :

Patent Use Description :

Patent Expiration Date : 2041-06-04

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10

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Compamed
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LENACAPAVIR SODIUM

US Patent Number : 10654827

Drug Substance Claim :

Drug Product Claim :

Application Number : 215973

Patent Use Code : U-3507

Delist Requested :

Patent Use Description :

Patent Expiration Date : 2037-08-17

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US Exclusivities

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