Home Immunology & Inflammation gp120/CD4 inhibitor Fostemsavir

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Fostemsavir gp120/CD4 inhibitor

Cat.No.S7220

Fostemsavir (BMS-663068, Rukobia), the phosphonooxymethyl prodrug of BMS626529, is an attachment inhibitor that targets HIV-1 gp120 and prevents its binding to CD4+ T cells with EC50 of < 10 nM.
Fostemsavir gp120/CD4 inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 583.49

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Quality Control

Batch: S722001 DMSO]100 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.65%
99.65

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (171.38 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

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In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
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Chemical Information, Storage & Stability

Molecular Weight 583.49 Formula

C25H26N7O8P

 Storage (From the date of receipt)
CAS No. 864953-29-7 -- Storage of Stock Solutions

Synonyms BMS-663068, Rukobia SMILES COC1=CN=C([N]2C=NC(=N2)C)C3=C1C(=C[N]3CO[P](O)(O)=O)C(=O)C(=O)N4CCN(CC4)C(=O)C5=CC=CC=C5

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Mechanism of Action

Targets/IC50/Ki
HIV-1 gp120
(Cell-free assay)
10 nM(EC50)
In vivo

BMS-663068 is the phosphonooxymethyl prodrug of BMS-626529 designed to increase the solubility of the compound in the gut. BMS-663068 is cleaved by alkaline phosphatase, located on the luminal surface of the small intestine brush border membranes, releasing BMS-626529. Due to its good membrane permeability, BMS-626529 is then rapidly absorbed. BMS-663068 is an orally active inhibitor of HIV-1 attachment.
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2026-08-14)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT07393659 RECRUITING
HIV Infections
ViiV Healthcare
 2026-07-21 PHASE3
NCT04648280 ACTIVE_NOT_RECRUITING
HIV Infections With Multi Drug Resistant Virus
PENTA Foundation
 2022-06-30 PHASE1; PHASE2
NCT07030920 RECRUITING
Human Immunodeficiency Virus (HIV); Cardiovascular Risk Factor
Centre hospitalier de l'Université de Montréal (CHUM)
 2025-09-30 PHASE2
NCT07053384 ACTIVE_NOT_RECRUITING
HIV Infections
ViiV Healthcare
 2025-07-10 PHASE1
NCT05220358 ACTIVE_NOT_RECRUITING
HIV-1-infection
Orlando Immunology Center
 2022-06-15 PHASE4
NCT04648280 Recruiting
HIV Infections With Multi Drug Resistant Virus
PENTA Foundation|ViiV Healthcare|PHPT Foundation|Hospital Universitario 12 de Octubre|Cromsource
 2022-06-30 Phase 1|Phase 2

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