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bictegravir

Trade name: Biktarvy

Small moleculeapprovedOrphan Drug FDA

Approved

Feb 7, 2018

Bictegravir is a component of the fixed-dose combination product bictegravir/emtricitabine/tenofovir alafenamide (BIKTARVY®), which received marketing approval for the treatment of human immunodeficiency virus (HIV) infection by the U.S. Food and Drug Administration in February 2018. Bictegravir inhibits the strand transfer activity of HIV-1 integrase, an HIV-1 encoded enzyme that is required for viral replication. Inhibition of integrase prevents the integration of linear HIV-1 DNA into host genomic DNA, blocking the formation of the HIV-1 provirus and propagation of the virus. — NCATS

Clinical trial activity

101 trials · 86 clinical orgs · 1 marketing orgs

Phase 1
12
Phase 2
36
Phase 3
32
Phase 4
44

Earliest trial started Oct 1, 2014 (NCT02275065)

Timeline

2010s

  1. Jan 1, 2014

    Gilead Sciences — Earliest Phase 1 Sponsor(trial)

  2. Jan 1, 2015

    Gilead Sciences — Earliest Phase 2 Sponsor(trial)

  3. Jan 1, 2015

    Gilead Sciences — Earliest Phase 3 Sponsor(trial)

  4. May 17, 2017

    Orphan Drug Designation

  5. Feb 7, 2018

    Gilead Sciences — Earliest FDA Approval

  6. Feb 7, 2018

    Gilead Sciences — NDA Secondary Org

  7. Feb 7, 2018

    Gilead Sciences — NDA Organization

Indications

Approved for

Studied for

Mechanism of action

Combination products

  • biktarvy

    with emtricitabine, tenofovir alafenamide

    Also known as bictegravir, embitcitabine, tenofovir alafenamide, bictegravir/emtricitabine/tenofovir alafenamide 50/200/25 mg

Approval history

  • approvedPriority reviewFeb 7, 2018

Chemistry & pharmacology

Loading structure…

SMILES

O=C(NCc1c(F)cc(F)cc1F)c1cn2c(c(O)c1=O)C(=O)N1[C@H]3CC[C@H](C3)O[C@@H]1C2
Mol. weight
449.39 g/mol
Lipinski Ro5
Pass
Rule of 3
No
Chirality
Single Stereoisomer
Inorganic
No
Polymer
No
Delivery
Oral
Availability
Prescription Only

Oral

Yes

Parenteral

No

Topical

No

Sources

Also known as

  • bictegravir
  • bictegravir
  • bictegravir
  • gs-9883
  • gs-9883

Clinical trials

NCT IDPhaseStart dateSponsor(s)
NCT07055451Phase 1Aug 12, 2025Gilead Sciences
NCT07115368Phase 1Aug 11, 2025Gilead Sciences
NCT07001319Phase 1May 29, 2025Gilead Sciences
NCT07075146Phase 3May 5, 2025Instituto Mexicano del Seguro Social
NCT06891066Phase 2Apr 14, 2025Merck
NCT07031063Phase 4Apr 1, 2025Instituto Mexicano del Seguro Social
NCT06830668Phase 4Feb 28, 2025Gilead Sciences, Government of China
NCT06532656Phase 2/Phase 3 (Phase 3)Nov 30, 2024Gilead Sciences
NCT06613685Phase 2/Phase 3 (Phase 3)Oct 21, 2024Gilead Sciences
NCT06630286Phase 3Oct 9, 2024Gilead Sciences
NCT06465862N/ASep 15, 2024Gilead Sciences, Harvard University
NCT06337032Phase 4Aug 27, 2024Gilead Sciences
NCT06544733Phase 2/Phase 3 (Phase 3)Aug 20, 2024Gilead Sciences
NCT06375304Phase 4May 1, 2024McGill University
NCT06374758Phase 4Apr 29, 2024Gilead Sciences, University of Missouri
NCT06356194Phase 1Apr 15, 2024Atea Pharmaceuticals, Inc.
NCT06333808Phase 3Mar 25, 2024Gilead Sciences
NCT05979311Phase 3Dec 29, 2023ViiV Healthcare
NCT06104306Phase 4Dec 13, 2023Gilead Sciences
NCT05705349Phase 3Mar 8, 2023Merck
Showing 20 of 101 trials
Page 1 / 6

Organizations

Research & Development (86)

OrganizationOrg typeTrialsAs lead sponsorPhasesEarliest year
Gilead SciencesFor profit503052014
MerckFor profit10632020
Janssen Pharmaceutica NVFor profit5232019
ViiV HealthcareFor profit5222020
Fundacion SEIMC-GESIDAAcademic/Hospital4412019
Harvard UniversityAcademic/Hospital4332018
University of BarcelonaAcademic/Hospital4332020
Institut de Médecine et d'Epidémiologie Appliquée - Fondation Internationale Léon M'BaAcademic/Hospital3322019
Instituto Mexicano del Seguro SocialGovernment3332021
University of LondonAcademic/Hospital3332020
Boston UniversityAcademic/Hospital2022018
Cornell UniversityAcademic/Hospital2112020
Emory UniversityAcademic/Hospital2212019
Imperial College LondonAcademic/Hospital2022020
Johns Hopkins UniversityAcademic/Hospital2122019
National Institute of Allergy and Infectious Diseases (NIAID)Government2122020
University of British ColumbiaAcademic/Hospital2112018
Analysis Group, Inc.For profit1012020
Atea Pharmaceuticals, Inc.For profit1112024
Azienda Ospedaliera Universitaria SeneseAcademic/Hospital1112019
86 organizations
Page 1 / 5

Marketing (2)

OrganizationOrg typeRelationshipDate
Gilead SciencesFor profitNDA2Feb 7, 2018
Gilead SciencesFor profitNDAFeb 7, 2018