Lenacapavir

Highest phase reached
Drug type
Small molecule
First approval year

First approval year
Listing at source
Listed
Highest phase reached

Drug type
Small molecule
Drug name
Lenacapavir
Molecular weight
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

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)

Approved for (1)

In development for (1)