Lenacapavir
Highest phase reached
Approved
Drug type
Small molecule
First approval year
2022
- First approval year
- 2022
- Listing at source
- Listed
- Highest phase reached
- Approved
- Drug type
- Small molecule
- Drug name
- Lenacapavir
- Molecular weight
- 968.3
- Structure (SMILES)
- CC(C)(C#Cc1ccc(-c2ccc(Cl)c3c(NS(C)(=O)=O)nn(CC(F)(F)F)c23)c([C@H](Cc2cc(F)cc(F)c2)NC(=O)Cn2nc(C(F)(F)F)c3c2C(F)(F)[C@@H]2C[C@H]32)n1)S(C)(=O)=O
- gs 6207
- gs 714207
- gs ca 2
- gs ca1
- gs ca2
- gs hiv
- GS-6207
- GS-714207
- GS-CA-2
- GS-CA1
- GS-CA2
- GS-HIV
- gs6207
- GS6207
- lenacapavir
- Lenacapavir
- lenacapavir [INN]
- Lenacapavir [MI]
- LENACAPAVIR [USAN]
- Lenacapavir [WHO-DD]
- lenacapavir inn
- lenacapavir mi
- lenacapavir usan
- lenacapavir who dd
- CAS registry numbers
- 2189684-44-2
- ChEMBL ID
- CHEMBL4594438
- InChIKey
- BRYXUCLEHAUSDY-WEWMWRJBSA-N
- PubChem compound IDs
- 133082658
- RxNorm IDs (RxCUI)
- 2625651
- FDA ingredient codes (UNII)
- A9A0O6FB4H
- J05AX
- J05AX31
Sources for recorded values
- Applicant
- GILEAD SCIENCES INC
- Approval date
- 22 Dec 2022
- Application number
- NDA215973
- Status
- Authorised
- Status date
- 17 Aug 2022
- Authorisation date
- 17 Aug 2022
- Approved indications
- 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).
- Product number
- EMEA/H/C/005638
- Authorisation holder
- Gilead Sciences Ireland Unlimited Company
- Priority medicines scheme
- No
- Generic
- No
- Biosimilar
- No
- Generic medicines
- 0
- Biosimilar medicines
- 0
- Advanced therapy
- No
- Conditional approval
- No
- Additional monitoring
- Yes
- Accelerated assessment
- No
- Exceptional circumstances
- No
Therapeutic areas
- HIV Infections
European medicines record
- Patents
- 0
- Designations
- 5
- First in class
- Yes
- Fast track
- Yes
- Breakthrough designation
- Yes
- Orphan designation
- No
- Priority review
- Yes
- Orphan exclusivity
- No
- Accelerated approval
- No
- Availability
- Prescription only
- United States (FDA)
- Approved
- European Union (EMA)
- Authorised
- Pharmacology name
- lenacapavir
- Type
- Synthetic organic
- Drug name stem
- -vir
- Approval recorded by Guide to Pharmacology
- Yes
Administration routes
- Oral
- Parenteral
Mechanisms of action
- Mechanism
- Structural capsid protein inhibitor
- Action type
- Inhibitor
- Target
- Structural capsid protein
- Protein identifier
- Q76129
Open Targets mechanisms
- Mechanism
- Structural capsid protein inhibitor
- Action type
- Inhibitor
- Target
- Structural capsid protein
- Condition
- HIV Infections
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000180
- Subject identifier
- D015658
- Condition
- Virus Diseases
- Highest recorded phase
- 4
- Condition identifier
- EFO:0000763
- Subject identifier
- D014777
- Condition
- HIV Infections
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000764
- Subject identifier
- D015658
- Condition identifier
- EFO_0000180
- Highest recorded phase
- 3
- Condition identifier
- EFO_0000763
- Condition identifier
- EFO_0000764
- Condition identifier
- MONDO_0005108
- Highest recorded phase
- 4
- Condition identifier
- MONDO_0005109
- Highest recorded phase
- 4
- Event
- labelled drug-drug interaction medication error
- Reports
- 8
- Reporting signal score
- 45.6173
- Event
- product use in unapproved therapeutic environment
- Reports
- 8
- Reporting signal score
- 74.2985
- Event
- single component of a two-component product administered
- Reports
- 4
- Reporting signal score
- 40.6239
- NCT03739866
- NCT04143594
- NCT04150068
- NCT04811040
- NCT05502341
- NCT06333808
- NCT04925752
- NCT04994509
- NCT05729568
- NCT06101329
- NCT06101342
- Dose
- 927 mg
- Route
- Subcutaneous
- How often
- Every 6 months
Conditions of use
- Administer into the abdomen by healthcare provider
- Hydrogen bond acceptors
- 10
- Hydrogen bond donors
- 2
- Polar surface area
- 157.94
- Calculated partition coefficient (ALogP)
- 7.66
- Calculated partition coefficient (XLogP)
- 6.4
- Prodrug
- No
- Chirality
- Single enantiomer
- Inorganic
- No
- Rule-of-five violations
- 2
- Rotatable bonds
- 11
- Heavy atoms
- 64
- Molecular formula
- C39H32ClF10N7O5S2
- Monoisotopic mass
- 967.1435188
- Natural product
- No
- Recorded assays
- 63
- Active assays
- 9
Active assay types
- Confirmatory
Related records
Trials (26)
- A Study of GS-3242 in Combination With Lenacapavir Versus Biktarvy in Virologically Suppressed People With HIV-1
- A Study of Teropavimab and Zinlirvimab in Combination With Capsid Inhibitor Lenacapavir in Virologically Suppressed Adults With HIV-1 Infection
- ALIGN: A Non-randomised Study Delivering Injectable Lenacapavir for HIV Prevention Within a Pre-exposure Prophylaxis (PrEP) Choice Context in Cape Town, South Africa.
- CAbotégravir LENacapavir DUal Long Acting
- Evaluation of Long-Acting Lenacapavir for the Treatment of HIV-1 in Treatment-experienced Adolescents and Children
- Implementation Study of Lenacapavir Pre-exposure Prophylaxis for HIV Prevention
- Lenacapavir Intensification to Disrupt HIV Reservoirs in Virologically Suppressed People With HIV Receiving Antiretroviral Therapy
- Mobile Vehicle-Based Delivery of Lenacapavir Pre-Exposure Prophylaxis in Los Angeles County
- Pre-Exposure Prophylaxis Study of Lenacapavir and Emtricitabine/Tenofovir Alafenamide in Adolescent Girls and Young Women at Risk of HIV Infection
- Pre-Exposure Prophylaxis Study of Lenacapavir in Cisgender Men, Transgender Women, Transgender Men, and Gender Nonbinary People at Risk for HIV Infection
- Real World Use of Lenacapavir, as an add-on to an Optimized Background Regimen in France
- Study of an Injectable Regimen of GS-3242 With Lenacapavir Compared to Biktarvy in People New to HIV-1 Treatment
- Study of Bictegravir/Lenacapavir in Children and Adolescents With HIV-1
- Study of Lenacapavir and Emtricitabine/Tenofovir Disoproxil Fumarate (F/TDF) for Prevention of HIV in People Who Inject Drugs (HPTN 103)
- Study of Lenacapavir and Emtricitabine/Tenofovir Disoproxil Fumarate (F/TDF) in Prevention of HIV in Cisgender Women in the United States (HPTN 102)
- Study of Lenacapavir as a Once-Yearly Injection for HIV Pre-exposure Prophylaxis (PrEP)
- Study of Lenacapavir Taken Twice a Year for HIV Pre-Exposure Prophylaxis (PrEP)
- Study of Lenacapavir, Teropavimab, and Zinlirvimab in Virologically Suppressed Adults With HIV-1 on Stable Oral Treatment Regimens
- Study of Lenacapavir, Teropavimab, and Zinlirvimab Versus Cabotegravir and Rilpivirine in Virologically Suppressed Adults With HIV-1 on Oral Daily Antiretroviral Therapy
- Study to Compare Bictegravir/Lenacapavir Versus Current Therapy in People With HIV-1 Who Are Successfully Treated With a Complicated Regimen (ARTISTRY-1)
Approved for (1)
In development for (1)
- HIV infectious disease Phase 3