Bictegravir

Bictegravir

API’s Name:Bictegravir 1611493-60-7

CAS No.:1611493-60-7

Indication:HIV-1 infection

Innovator:Gilead Sciences

Specification:In-House

Patent Expiry Date(The U.S):Dec. 19, 2033

US DMF

EU DMF

CEP

Only for R&D purpose


Product Detail

Intermediates

Code

CAS

Specification

BTGM

1279032-31-3

In-House

BTGM2

214759-21-4

In-House



Description

Bictegravir is a novel, potent inhibitor of HIV-1 integrase with an IC50 of 7.5 nM.


In Vitro

Bictegravir (BIC) inhibits the strand transfer activity with an IC50 of 7.5± 0.3 nM. Relative to its inhibition of strand transfer activity, Bictegravir is a much weaker inhibitor of 3′-processing activity of HIV-1 IN, with an IC50 of 241±51 nM. Bictegravir enhances the accumulation of 2-LTR circles ~5-fold relative to the mock-treated control and reduces the amount of authentic integration products in infected cells by 100-fold. Bictegravir potently inhibits HIV-1 replication in both MT-2 and MT-4 cells with EC50s of 1.5 and 2.4 nM, respectively. Bictegravir exhibits potent antiviral effects in both primary CD4+ T lymphocytes and monocyte-derived macrophages, with EC50s of 1.5±0.3 nM and 6.6±4.1 nM, respectively, which are comparable to values obtained in T-cell lines[1].


MCE has not independently confirmed the accuracy of these methods. They are for reference only.


NCT Number

Sponsor

Condition

Start Date

Phase

NCT03998176

University of Nebraska|Gilead Sciences

HIV-1-infection

October 9, 2019

Phase 4

NCT03789968

Thomas Jefferson University|University of Maryland, College Park|Indiana University Health|The Brooklyn Hospital Center|University of Illinois at Chicago|Nova Southeastern University|University of California, San Francisco

HIV+AIDS

September 1, 2019


NCT04249037

University of Colorado, Denver|Gilead Sciences

HIV+AIDS

March 1, 2020

Not Applicable

NCT04132674

Vancouver Infectious Diseases Centre

Human Immunodeficiency Virus I Infection|Drug Use

November 26, 2018

Phase 4

NCT04054089

Cristina Mussini|University of Modena and Reggio Emilia

HIV Infections

September 2019

Phase 4

NCT04155554

Azienda Ospedaliera Universitaria Senese|Catholic University of the Sacred Heart|Ospedale Policlinico San Martino|Azienda Ospedaliera San Paolo|Ospedale Amedeo di Savoia

HIV-1-infection

January 29, 2020

Phase 3

NCT02275065

Gilead Sciences

HIV-1 Infection

October 2014

Phase 1

NCT03711253

University of Southern California

Acute HIV Infection

October 14, 2019

Phase 4

NCT02400307

Gilead Sciences

HIV

April 17, 2015

Phase 1

NCT03499483

Fenway Community Health

HIV Prevention

January 24, 2019

Phase 4

NCT03502005

Midland Research Group, Inc.|Gilead Sciences

Human Immunodeficiency Virus

March 1, 2018

Phase 4


Chemical structur

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