Bictegravir

Summary

Bictegravir (CHEMBL3989866) is an approved small-molecule HIV-1 integrase inhibitor; indicated across 2 conditions including hiv infectious disease.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• Indications: 2 conditions
• Clinical trials: 27
• Chemistry: 449.4 Da · C21H18F3N3O5

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL3989866
Name	Bictegravir
Type	Small molecule
Max phase	4
FDA approved	no
PubChem CID	90311989
ChEBI	CHEBI:172943
Molecular formula	C21H18F3N3O5
Molecular weight	449.4
InChIKey	SOLUWJRYJLAZCX-LYOVBCGYSA-N

SMILES: C1C[C@@H]2C[C@H]1N3[C@H](O2)CN4C=C(C(=O)C(=C4C3=O)O)C(=O)NCC5=C(C=C(C=C5F)F)F

IUPAC name: (1S,11R,13R)-5-hydroxy-3,6-dioxo-N-[(2,4,6-trifluorophenyl)methyl]-12-oxa-2,9-diazatetracyclo[11.2.1.02,11.04,9]hexadeca-4,7-diene-7-carboxamide

ChEBI definition: A monocarboxylic acid amide obtained by formal condensation of the carboxy group of (2R,5S,13aR)-8-hydroxy-7,9-dioxo-2,3,4,5,7,9,13,13a-octahydro-2,5-methanopyrido[1’,2’:4,5]pyrazino[2,1-b][1,3]oxazepine-10-carboxylic acid with the amino group of 2,4,6-trifluorobenzylamine. It is a second-generation integrase strand transfer inhibitor (INSTI) and used (as its sodium salt) for the treatment of HIV-1.

Pharmacological roles (ChEBI): HIV-1 integrase inhibitor.

Also known as: Bictegravir, GS-9883, BICTEGRAVIR

Parent form; salt/anhydrous children: CHEMBL3989867

Patent coverage: 495 distinct patent families (1,306 SureChEMBL compound mentions), from 1 matched compound structure(s). Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Broader ChEMBL bioactivity targets: 1 (assay-derived). Sample: Solute carrier family 22 member 2.

Bioactivity

ChEMBL activities: 2 potent at pChembl ≥ 5 of 2 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
SLC22A2	6.31	IC50	487	nM	CHEMBL_ACT_27226358
SLC22A2	6.31	IC50	487	nM	CHEMBL_ACT_28901507

Target pathways

No target-pathway data for this drug (no mapped target genes).

Indications & clinical

Indications

2 indications (0 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).

Indication	Trial phase	MONDO	EFO
HIV infectious disease	3	MONDO:0005109	EFO:0000180

1 further indication record had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 27.

Phase distribution

Phase	Trials
PHASE4	10
Not specified	7
PHASE3	3
PHASE2/PHASE3	3
PHASE1	3
PHASE2	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT06374758	PHASE4	RECRUITING	Accelerated ART Initiation for PWHIV Who Are Out of Care
NCT03499483	PHASE4	COMPLETED	Biktarvy for Non-Occupational Post-Exposure Prophylaxis (nPEP)
NCT03502005	PHASE4	COMPLETED	Efficacy, Safety & Tolerability of Switching EFV/TDF/FTC to BIC/FTC/TAF in Virologically Suppressed Adults With HIV-1
NCT03711253	PHASE4	UNKNOWN	Empiric Treatment for Acute HIV in the ED
NCT03998176	PHASE4	COMPLETED	Bictegravir/Emtricitabine/Tenofovir Alafenamide (B/F/TAF) in HIV-1 Infected Patients With Active Illicit Substance usE
NCT04132674	PHASE4	UNKNOWN	Switching to a Fixed Dose Combination of Bictegravir/Emtricitabine/Tenofovir Alafenamide (B/F/TAF) in HIV-1 Infected Marginalized Populations Who Are Virologically Suppressed
NCT04249037	PHASE4	TERMINATED	Rapid Start vs. Standard Start Antiretroviral Therapy (ART) in HIV
NCT04538040	PHASE4	COMPLETED	Bictegravir/Emtricitabine/Tenofovir Alafenide Plus Doravirine
NCT04585737	PHASE4	COMPLETED	Efficacy of Switching to DTG/3TC in Virologically-suppressed Adults Currently on B/F/TAF
NCT04884139	PHASE4	COMPLETED	DTG/3TC vs. BIC/FTC/TAF Maintenance Therapy in People Living With HIV:
NCT05502341	PHASE2/PHASE3	ACTIVE_NOT_RECRUITING	Study to Compare Bictegravir/Lenacapavir Versus Current Therapy in People With HIV-1 Who Are Successfully Treated With a Complicated Regimen
NCT05979311	PHASE3	ACTIVE_NOT_RECRUITING	A Study to Evaluate the Efficacy, Safety, and Tolerability of Using an Oral Once-daily 2 Drug Regimen Compared to an Oral Once-daily 3 Drug Regimen for the Treatment of Human Immunodeficiency Virus (HIV)-1 in Adults Who Have Not Previously Taken Antiretroviral Therapy
NCT06333808	PHASE3	ACTIVE_NOT_RECRUITING	Study to Compare Bictegravir/Lenacapavir Versus Current Therapy in People With HIV-1 Who Are Successfully Treated With Biktarvy
NCT06544733	PHASE2/PHASE3	ACTIVE_NOT_RECRUITING	Study of Oral Weekly Lepetegravir (Formerly GS-1720) and Lenacapavir Pacfosacil (Formerly GS-4182) Versus Biktarvy in People With HIV-1 Who Are Virologically Suppressed
NCT04155554	PHASE3	UNKNOWN	Neurological Monitoring in Patients Switching From Dolutegravir Based Regimen to Bictegravir Based Regimen
NCT06613685	PHASE2/PHASE3	TERMINATED	Study of Oral Weekly GS-1720 and GS-4182 Compared With Biktarvy in People With HIV-1 Who Have Not Been Treated
NCT04483674	PHASE2	UNKNOWN	Bictegravir/FTC/TAF for the Treatment of Primary HIV Infection
NCT07532304	PHASE1	RECRUITING	A Clinical Trial of MK-4646 With Bictegravir/Emtricitabine/Tenofovir Alafenamide and Dolutegravir in Healthy Adult Participants (MK-4646)
NCT02275065	PHASE1	COMPLETED	Study to Evaluate Safety, Pharmacokinetics, and Antiviral Activity of Bictegravir (GS-9883) in Human Immunodeficiency Virus (HIV)-1 Infected Participants
NCT02400307	PHASE1	COMPLETED	Pharmacokinetics of Bictegravir in Adults With Normal and Impaired Renal Function
NCT03789968	Not specified	COMPLETED	The Incidence and Severity of Drug Interactions Before and After Switching Antiretroviral Therapy to Bictegravir/Emtricitabine/Tenofovir Alafenamide in Treatment Experienced Patients
NCT04518228	Not specified	COMPLETED	Pharmacokinetic Properties of Antiretroviral and Anti-Tuberculosis Drugs During Pregnancy and Postpartum
NCT04712058	Not specified	UNKNOWN	Same-day Antiretroviral Therapy With BIC/F/TAF
NCT04805944	Not specified	COMPLETED	Gut Microbiota, PGx and INSTIs Response
NCT05526118	Not specified	UNKNOWN	Advanced HIV: Outcomes for Rapid ART
NCT06629480	Not specified	COMPLETED	Incidence of Metabolic Syndrome in People Living With HIV Without ExperienCe to ART Who Start DoLutegravir Based-Regimen Compared With BictegrAvir Based-RegimeN
NCT07004933	Not specified	COMPLETED	Rapid Antiretroviral Treatment Initiation With BIC/FTC/TAF in HIV-infected People Who Inject Drugs (PWID)

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline or drug-level clinical/variant annotations in PharmGKB for this molecule.

Related molecules

Related molecules

No competitor molecules sharing a primary target (ChEMBL phase ≥2 or PubChem drug-class).