VH3739937 / GSK, ViiV Healthcare - LARVOL DELTA

A Study to Investigate the Antiviral Effect, Safety, Tolerability and Pharmacokinetics of VH3739937 in in Treatment-Naive Adults Living With HIV-1 (clinicaltrials.gov) - P2 | N=21 | Terminated | Sponsor: ViiV Healthcare | Suspended ➔ Terminated; Sponsor decision

Trial termination • Human Immunodeficiency Virus • Infectious Disease

VH3739937 Phase 1 Multiple Ascending Dose (MAD) Study in Healthy Volunteers Including Relative Bioavailability (RBA), Optional Food Effect (FE), and Drug-drug Interaction (DDI) (clinicaltrials.gov) - P1 | N=0 | Withdrawn | Sponsor: ViiV Healthcare | N=67 ➔ 0 | Trial completion date: Jan 2026 ➔ Aug 2024 | Suspended ➔ Withdrawn | Trial primary completion date: Jan 2026 ➔ Aug 2024

Enrollment change • Trial completion date • Trial primary completion date • Trial withdrawal • Human Immunodeficiency Virus • Infectious Disease

Invention of VH-937, a Potent HIV-1 Maturation Inhibitor with the Potential for Infrequent Oral Dosing in Humans. (PubMed, ACS Med Chem Lett) - "VH3739937, (VH-937, 24) is an advanced HIV-1 maturation inhibitor (MI) with a 4-cyanopyridyl ether replacing the fluorine present in the previous lead MI GSK3640254 (GSK254, 3). Structure-activity optimization led to the invention of VH-937, which combined the best overall antiviral profile with pharmacokinetic properties in animal models. These properties indicate the potential for infrequent dosing, a finding confirmed in initial clinical studies in humans that suggests its potential as a once-weekly dosing agent."

Journal • Human Immunodeficiency Virus • Infectious Disease

Preclinical Profile of the HIV-1 Maturation Inhibitor VH3739937. (PubMed, Viruses) - "Measured dissociation rates from wild-type and A364V-containing VLPs help explain resistance to the A364V mutation. Overall, the in vitro antiviral activity of VH-937 supports its continued development as a treatment for HIV-1."

Journal • Preclinical • Human Immunodeficiency Virus • Infectious Disease

A Study to Investigate the Antiviral Effect, Safety, Tolerability and Pharmacokinetics of VH3739937 in in Treatment-Naive Adults Living With HIV-1 (clinicaltrials.gov) - P2 | N=26 | Suspended | Sponsor: ViiV Healthcare | Trial completion date: Jun 2024 ➔ Nov 2024 | Not yet recruiting ➔ Suspended | Trial primary completion date: Jun 2024 ➔ Nov 2024

Trial completion date • Trial primary completion date • Trial suspension • Human Immunodeficiency Virus • Infectious Disease

VH3739937 Phase 1 Multiple Ascending Dose (MAD) Study in Healthy Volunteers Including Relative Bioavailability (RBA), Optional Food Effect (FE), and Drug-drug Interaction (DDI) (clinicaltrials.gov) - P1 | N=67 | Suspended | Sponsor: ViiV Healthcare | Trial completion date: Mar 2025 ➔ Jan 2026 | Not yet recruiting ➔ Suspended | Trial primary completion date: Mar 2025 ➔ Jan 2026

Trial completion date • Trial primary completion date • Trial suspension • Human Immunodeficiency Virus • Infectious Disease

Current status of the small molecule anti-HIV drugs in the pipeline or recently approved. (PubMed, Bioorg Med Chem) - "These compounds include analogues of nucleoside reverse transcriptase inhibitors (NRTIs) - islatravir and censavudine; non-nucleoside reverse transcriptase inhibitors (NNRTIs) - Rilpivirine, elsulfavirine and doravirine; integrase inhibitors namely cabotegravir and dolutegravir and chemokine coreceptors 5 and 2 (CC5/CCR2) antagonists for example cenicriviroc. Also, fostemsavir is being developed as an attachment inhibitor while lenacapavir, VH4004280 and VH4011499 are capsid inhibitors. Others are maturation inhibitors such as GSK-254, GSK3532795, GSK3739937, GSK2838232, and other compounds labelled as miscellaneous (do not belong to the classical groups of anti-HIV drugs or to the newer classes) such as obefazimod and BIT225. There is a considerable progress in the development of new anti-HIV drugs and the effort will continue since HIV infections has no cure or vaccine till now. Efforts are needed to reduce the toxicity of available drugs or discover new drugs with new..."

Journal • Review • Human Immunodeficiency Virus • Infectious Disease • CCR2

VH3739937 Phase 1 Multiple Ascending Dose (MAD) Study in Healthy Volunteers Including Relative Bioavailability (RBA), Optional Food Effect (FE), and Drug-drug Interaction (DDI) (clinicaltrials.gov) - P1 | N=91 | Not yet recruiting | Sponsor: ViiV Healthcare

New P1 trial • Human Immunodeficiency Virus • Infectious Disease

The Preclinical Profile of Maturation Inhibitor VH3739937 (CROI 2024) - "Background: VH3739937 (VH937) is a next generation maturation inhibitor (MI) currently in clinical trials. The pre-clinical virology profile of VH937 supported the progression of this MI into clinical development."

Preclinical • Human Immunodeficiency Virus • Infectious Disease

A Study to Investigate the Antiviral Effect, Safety, Tolerability and Pharmacokinetics of VH3739937 in in Treatment-Naive Adults Living With HIV-1 (clinicaltrials.gov) - P2 | N=26 | Not yet recruiting | Sponsor: ViiV Healthcare

New P2 trial • Human Immunodeficiency Virus • Infectious Disease

A phase I, first-in-human study investigating the safety, tolerability, and pharmacokinetics of the maturation inhibitor GSK3739937. (PubMed, Pharmacol Res Perspect) - P1 | "Pharmacokinetic parameters of long half-life and accumulation of exposure following repeat dosing suggest the potential for weekly oral dosing. ClinicalTrials.gov identifier: NCT04493684."

Journal • P1 data • PK/PD data • Gastrointestinal Disorder • Human Immunodeficiency Virus • Infectious Disease

GSK3739937 First-Time-In-Human (FTIH) Study in Healthy Volunteers (clinicaltrials.gov) - P1; N=91; Completed; Sponsor: ViiV Healthcare; Recruiting ➔ Completed

Clinical • Trial completion • Human Immunodeficiency Virus • Infectious Disease • PCR

GSK3739937 First-Time-In-Human (FTIH) Study in Healthy Volunteers (clinicaltrials.gov) - P1; N=76; Recruiting; Sponsor: ViiV Healthcare; N=48 ➔ 76

Clinical • Enrollment change • Human Immunodeficiency Virus • Infectious Disease • PCR

GSK3739937 First-Time-In-Human (FTIH) Study in Healthy Volunteers (clinicaltrials.gov) - P1; N=48; Not yet recruiting; Sponsor: ViiV Healthcare

Clinical • New P1 trial • Human Immunodeficiency Virus • Infectious Disease • PCR

GSK3739937 First-Time-In-Human (FTIH) Study in Healthy Volunteers (clinicaltrials.gov) - P1; N=48; Recruiting; Sponsor: ViiV Healthcare; Not yet recruiting ➔ Recruiting

Clinical • Enrollment open • Human Immunodeficiency Virus • Infectious Disease • PCR

GSK3739937 First-Time-In-Human (FTIH) Study in Healthy Volunteers (clinicaltrials.gov) - P1; N=48; Recruiting; Sponsor: ViiV Healthcare; Trial completion date: Feb 2021 ➔ Aug 2021; Trial primary completion date: Feb 2021 ➔ Aug 2021

Clinical • Trial completion date • Trial primary completion date • Human Immunodeficiency Virus • Infectious Disease • PCR