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[CAS NO. 1051375-10-0] Cabotegravir

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Catalog:	HY-15592
Brand:	MCE
CAS:	1051375-10-0

Overview

MDL	MFCD25976748
Molecular Weight	405.35
Molecular Formula	C19H17F2N3O5
SMILES	FC1=C(CNC(C2=CN3C(C(N([C@@H](C)CO4)[C@@]4([H])C3)=O)=C(O)C2=O)=O)C=CC(F)=C1

For research use only. We do not sell to patients.

5 Publications Citing Use of MCE

[1]J Infect Dis. 2022 Sep 19;jiac386.
[2]Antimicrob Agents Chemother. 2019 Dec 20;64(1):e01717-19.
[3]Int J Antimicrob Agents. 2019 Dec;54(6):814-819.
[4]Pharmaceutics. 2022, 14(9), 1761.
[5]Drug Metab Dispos. 2019 May;47(5):535-544.

Summary

Cabotegravir (GSK-1265744) is a orally active and long-acting HIV integrase strand transfer inhibitor and organic anion transporter 1/3 ( OAT1 / OAT3 ) inhibitor with IC ₅₀ values of 2.5 nM, 0.41 μM and 0.81 μM for HIV _ADA , OAT3 and OAT1, respectively. Cabotegravir is primarily metabolized by uridine diphosphate glucuronosyltransferase (UGT) 1A1, with low potential to interact with other antiretroviral drugs (ARVs). Cabotegravir can be used to research AIDS ^[1] ^[2] .

IC50 & Target

IC ₅₀ : 2.5 nM (HIV _ADA ) ^[1]
IC ₅₀ : 0.41 μM (OAT3), 0.81 μM (OAT1) ^[2]

In Vitro

Cabotegravir (GSK-1265744) inhibits the HIV-1 integrase catalyzed strand transfer reaction with an IC ₅₀ of 3.0 nM in vitro. The antiviral EC ₅₀ against HIV-1 Ba-L is 0.22 nM and that against NL432 is 0.34 nM in PBMCs, 0.57 nM using CellTiter-Glo and 1.3 nM using MTT in MT-4, and 0.5 nM in the PHIV assay, which uses a pseudotyped self-inactivating virus ^[3] .

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

Cell Viability Assay ^[3]

Cell Line:	MT-4 cells
Concentration:	0-32 nM
Incubation Time:	4 or 5 days
Result:	Showed antiviral activity with an EC ₅₀ of 1.3 nM.

In Vivo

The half-life of Cabotegravir is up to 54 days in mice ^[1] .
Cabotegravir (25 or 50 mg/kg; i.v.; single dose or twice) protects Macaques against intravenous challenge with SIVmac251 ^[4] .

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

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT04692077	National Institute of Allergy and Infectious Diseases (NIAID)	HIV Infections	February 19, 2020	Phase 2
NCT02159131	ViiV Healthcare	Infections, Human Immunodeficiency Virus and Hepatitis	August 2014	Phase 1
NCT04371380	ViiV Healthcare\|Janssen Pharmaceuticals\|GlaxoSmithKline	HIV Infections	September 16, 2020	Phase 1
NCT02720094	National Institute of Allergy and Infectious Diseases (NIAID)\|ViiV Healthcare\|Gilead Sciences	HIV Infections	December 2016	Phase 2\|Phase 3
NCT05515770	Evandro Chagas National Institute of Infectious Disease\|Beatriz Grinsztejn\|Thiago Torres\|Valdilea Gonçalves\|Brenda Hoagland	HIV Infections	September 20, 2022	Phase 3
NCT04542070	ViiV Healthcare\|Janssen, LP	HIV Infections	November 9, 2020	Phase 3
NCT03299049	ViiV Healthcare\|Janssen Research and Development	HIV Infections	October 27, 2017	Phase 3
NCT05374525	ViiV Healthcare	HIV Infections	May 18, 2022	Phase 4
NCT03739996	National Institute of Allergy and Infectious Diseases (NIAID)\|ViiV Healthcare	HIV Infections	December 31, 2019	Phase 2
NCT02027454	ViiV Healthcare\|GlaxoSmithKline	Infection, Human Immunodeficiency Virus	January 2014	Phase 1
NCT05514509	ViiV Healthcare	HIV Infections	October 31, 2022	Phase 4
NCT01648257	ViiV Healthcare	Infections, Human Immunodeficiency Virus and Hepatitis	August 2012	Phase 1
NCT02354950	ViiV Healthcare\|GlaxoSmithKline	HIV Infections	June 22, 2015	Phase 1
NCT00659191	GlaxoSmithKline	HIV Infection	February 2008	Phase 1
NCT05549726	University of California, San Francisco\|Infectious Diseases Research Collaboration, Uganda\|Makerere University\|Kenya Medical Research Institute\|University of California, Berkeley\|National Institute of Allergy and Infectious Diseases (NIAID)\|National Institute on Alcohol Abuse and Alcoholism (NIAAA)\|National Institute of Mental Health (NIMH)\|National Heart, Lung, and Blood Institute (NHLBI)\|ViiV Healthcare\|University of Pittsburgh	HIV	November 1, 2022	Phase 4
NCT01467531	ViiV Healthcare\|Shionogi	Infections, Human Immunodeficiency Virus and Hepatitis	November 2011	Phase 1
NCT02478463	ViiV Healthcare	Infection, Human Immunodeficiency Virus\|HIV Infections	February 27, 2017	Phase 1
NCT02354937	ViiV Healthcare	Infection, Human Immunodeficiency Virus\|HIV Infections	July 13, 2015	Phase 1
NCT02938520	ViiV Healthcare\|Janssen Pharmaceuticals\|GlaxoSmithKline	HIV Infections\|Glycogen Storage Disease Type II	October 27, 2016	Phase 3
NCT02951052	ViiV Healthcare\|Janssen Pharmaceuticals\|GlaxoSmithKline	Infection, Human Immunodeficiency Virus\|HIV Infections	October 28, 2016	Phase 3
NCT04518228	National Institute of Allergy and Infectious Diseases (NIAID)\|International Maternal Pediatric Adolescent AIDS Clinical Trials Group\|Eunice Kennedy Shriver National Institute of Child Health and Human Development (NICHD)\|National Institute of Mental Health (NIMH)\|Gilead Sciences\|ViiV Healthcare\|Merck Sharp & Dohme LLC	HIV Infections\|Tuberculosis	June 8, 2021
NCT00812318	ViiV Healthcare\|Shionogi\|GlaxoSmithKline	HIV Infection\|Infection, Human Immunodeficiency Virus	June 2008	Phase 1
NCT02462772	Centre for the AIDS Programme of Research in South Africa\|ViiV Healthcare	Human Immunodeficiency Virus	October 2015	Phase 2
NCT04484337	ViiV Healthcare	HIV Infections	July 31, 2020	Phase 1
NCT02178800	National Institute of Allergy and Infectious Diseases (NIAID)	HIV Infections	February 2015	Phase 2
NCT01756131	ViiV Healthcare\|GlaxoSmithKline	Infections, Human Immunodeficiency Virus and Herpesviridae	September 2010	Phase 1
NCT02799264	ViiV Healthcare\|Glaxosmithkline+Quintiles	Infection, Human Immunodeficiency Virus	June 2016	Phase 1
NCT05418868	ViiV Healthcare	HIV Infections	June 14, 2022	Phase 1
NCT04824131	National Institute of Allergy and Infectious Diseases (NIAID)	HIV Infections	November 4, 2020	Phase 2
NCT02345707	ViiV Healthcare	Infection, Human Immunodeficiency Virus	March 2015	Phase 1
NCT00920296	GlaxoSmithKline	Healthy Subjects\|Infection, Human Immunodeficiency Virus	July 2009	Phase 1
NCT03149848	ViiV Healthcare\|GlaxoSmithKline	Infection, Human Immunodeficiency Virus\|HIV Infections	June 6, 2017	Phase 1
NCT03497676	National Institute of Allergy and Infectious Diseases (NIAID)\|ViiV Healthcare	HIV Infections	March 19, 2019	Phase 1\|Phase 2
NCT01593046	ViiV Healthcare\|GlaxoSmithKline	Infection, Human Immunodeficiency Virus	May 2012	Phase 1
NCT00920426	ViiV Healthcare\|Shionogi\|GlaxoSmithKline	Infection, Human Immunodeficiency Virus	June 9, 2009	Phase 2
NCT01754116	ViiV Healthcare\|GlaxoSmithKline	Infection, Human Immunodeficiency Virus	January 2013	Phase 1
NCT02059031	ViiV Healthcare	Infection, Human Immunodeficiency Virus	February 2014	Phase 1
NCT01641809	ViiV Healthcare\|GlaxoSmithKline	Infection, Human Immunodeficiency Virus\|HIV Infections	August 6, 2012	Phase 2

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 16.67 mg/mL ( 41.12 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.4670 mL	12.3350 mL	24.6700 mL
5 mM	0.4934 mL	2.4670 mL	4.9340 mL
10 mM	0.2467 mL	1.2335 mL	2.4670 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 1.67 mg/mL (4.12 mM); Clear solution

* All of the co-solvents are available by MCE.

References

[1] Zhou T, et al. Creation of a nanoformulated cabotegravir prodrug with improved antiretroviral profiles. Biomaterials. 2018 Jan;151:53-65.
[2] Reese MJ, et al. Drug interaction profile of the HIV integrase inhibitor cabotegravir: assessment from in vitro studies and a clinical investigation with midazolam. Xenobiotica. 2015 Sep 4:1-12.
[3] Yoshinaga T, et al. Antiviral characteristics of GSK1265744, an HIV integrase inhibitor dosed orally or by long-acting injection. Antimicrob Agents Chemother. 2015 Jan;59(1):397-406.
[4] Andrews CD, et al. Cabotegravir long acting injection protects macaques against intravenous challenge with SIVmac251. AIDS. 2017 Feb 20;31(4):461-467.

Synonyms

Oxazolo[3,2-a]pyrido[1,2-d]pyrazine-8-carboxamide, N-[(2,4-difluorophenyl)methyl]-2,3,5,7,11,11a-hexahydro-6-hydroxy-3-methyl-5,7-dioxo-, (3S,11aR)-

(3S,11aR)-N-[(2,4-Difluorophenyl)methyl]-2,3,5,7,11,11a-hexahydro-6-hydroxy-3-methyl-5,7-dioxooxazolo[3,2-a]pyrido[1,2-d]pyrazine-8-carboxamide

Cabotegravir

GSK 1265744A

GSK 744

(3s,11Ar)-n-(2,4-difluorobenzyl)-6-hydroxy-3-methyl-5,7-dioxo-2,3,5,7,11,11a-hexahydrooxazolo[3,2-a]pyrido[1,2-d]pyrazine-8-carboxamide

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