VH4011499 / GSK, ViiV Healthcare - LARVOL DELTA

A Study to Assess the Safety, Tolerability, and Pharmacokinetics of VH4011499 Compared to Placebo in Adults Without HIV (clinicaltrials.gov) - P1 | N=168 | Recruiting | Sponsor: ViiV Healthcare | Trial primary completion date: Mar 2028 ➔ Aug 2028

Trial primary completion date • Human Immunodeficiency Virus • Infectious Disease

A Study to Evaluate the Safety, Tolerability, and Pharmacokinetics of a Single Suspension Injection of Investigational Capsid Inhibitors Compared to Placebo in Healthy Adults (clinicaltrials.gov) - P1 | N=208 | Recruiting | Sponsor: ViiV Healthcare | N=160 ➔ 208 | Trial completion date: May 2026 ➔ Sep 2026 | Trial primary completion date: May 2026 ➔ Sep 2026

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

Clinical Pharmacokinetics and Safety of Orally Administered VH4011499, a New HIV-1 Capsid Inhibitor, in Adults Without HIV. (PubMed, Infect Dis Ther) - P1 | "First-time-in-human data further characterize the pharmacokinetics of orally administered VH-499 and provide support for development of VH-499 as part of a complete long-acting regimen for HIV-1 treatment and prevention."

Journal • PK/PD data • Hematological Disorders • Human Immunodeficiency Virus • Infectious Disease • CYP3A4

Proof-of-Concept Trial of Oral VH4011499 (VH-499), a New HIV-1 Capsid Inhibitor (CROI 2025) - "A VH-499 exposure-response relationship was established. These results support further development of VH-499 as part of a complete long-acting regimen for the treatment of HIV-1."

Human Immunodeficiency Virus • Infectious Disease

A Study to Assess the Safety, Tolerability, and Pharmacokinetics of VH4011499 Compared to Placebo in Adults Without HIV (clinicaltrials.gov) - P1 | N=168 | Recruiting | Sponsor: ViiV Healthcare | Trial completion date: Mar 2028 ➔ Aug 2028

Trial completion date • Human Immunodeficiency Virus • Infectious Disease

A Study to Investigate the Effect of Food on the Bioavailability of a Capsid Inhibitor (CAI) in Male and Female Healthy Participants (clinicaltrials.gov) - P1 | N=60 | Completed | Sponsor: ViiV Healthcare | Recruiting ➔ Completed | N=36 ➔ 60 | Trial completion date: Jun 2024 ➔ Oct 2024 | Trial primary completion date: Jun 2024 ➔ Oct 2024

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

A Study to Assess the Safety, Tolerability, and Pharmacokinetics of VH4011499 Compared to Placebo in Adults Without HIV (clinicaltrials.gov) - P1 | N=168 | Recruiting | Sponsor: ViiV Healthcare | Not yet recruiting ➔ Recruiting

Enrollment open • Human Immunodeficiency Virus • Infectious Disease

A Study to Assess the Safety, Tolerability, and Pharmacokinetics of VH4011499 Compared to Placebo in Adults Without HIV (clinicaltrials.gov) - P1 | N=168 | Not yet recruiting | Sponsor: ViiV Healthcare

New P1 trial • Human Immunodeficiency Virus • Infectious Disease

CINNAMON: Proof of Concept Treatment Study of Orally Administered VH4004280 or VH4011499 in HIV-1 Infected Adults (clinicaltrials.gov) - P2 | N=44 | Completed | Sponsor: ViiV Healthcare | Active, not recruiting ➔ Completed

Monotherapy • Trial completion • Human Immunodeficiency Virus • Infectious Disease • CD4

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

Clinical pharmacokinetics and safety of orally administered VH4011499 (VH-499), a novel HIV-1 capsid inhibitor, in Adults Without HIV (AIDS 2024) - "We present the pharmacokinetics, drug interaction potential, and safety of VH-499 in a first-time-in-human study. This double-blind, randomized, placebo-controlled, phase 1 study evaluated oral VH-499 in healthy adults administered as single ascending doses as powder-in-bottle (PiB) and tablet (parts 1 and 3, respectively) and as multiple ascending doses as PiB for 14 days with or without midazolam (part 2), evaluating VH-499 inhibition/induction of CYP3A4. 73 participants were included (placebo, n=17; VH-499, n=56); 93% and 93% were male, 30% and 56% identified as Black or African American, and median age was 37 and 34 years in parts 1 and 3 and part 2, respectively. VH-499 was well tolerated, does not inhibit/induce CYP3A4, and exposures exceeded the anticipated therapeutic target across a range of single and multiple oral doses. These early data support further development of VH-499 as a long-acting antiretroviral for the treatment of HIV-1."

Clinical • PK/PD data • Dyslipidemia • Hematological Disorders • Human Immunodeficiency Virus • Infectious Disease • CYP3A4

Pre-clinical profiles of HIV-1 capsid inhibitors VH4004280 (VH-280) and VH4011499 (VH-499) (AIDS 2024) - "The pre-clinical virology profiles and other favorable drug-like properties of VH-280 and VH-499 support progression of these two CAIs into clinical development."

Preclinical • Human Immunodeficiency Virus • Infectious Disease

CINNAMON: Proof of Concept Treatment Study of Orally Administered VH4004280 or VH4011499 in HIV-1 Infected Adults (clinicaltrials.gov) - P2 | N=43 | Active, not recruiting | Sponsor: ViiV Healthcare | Recruiting ➔ Active, not recruiting

Enrollment closed • Monotherapy • Human Immunodeficiency Virus • Infectious Disease • CD4

A Study to Investigate the Effect of Food on the Bioavailability of a Capsid Inhibitor (CAI) in Male and Female Healthy Participants (clinicaltrials.gov) - P1 | N=36 | Recruiting | Sponsor: ViiV Healthcare | Not yet recruiting ➔ Recruiting

Enrollment open • Human Immunodeficiency Virus • Infectious Disease

A Study to Investigate the Effect of Food on the Bioavailability of a Capsid Inhibitor (CAI) in Male and Female Healthy Participants (clinicaltrials.gov) - P1 | N=36 | Not yet recruiting | Sponsor: ViiV Healthcare

New P1 trial • Human Immunodeficiency Virus • Infectious Disease

CINNAMON: Proof of Concept Treatment Study of Orally Administered VH4004280 or VH4011499 in HIV-1 Infected Adults (clinicaltrials.gov) - P2 | N=42 | Recruiting | Sponsor: ViiV Healthcare | Not yet recruiting ➔ Recruiting | Phase classification: P2a ➔ P2

Enrollment open • Monotherapy • Phase classification • Human Immunodeficiency Virus • Infectious Disease • CD4

A Study to Evaluate the Safety, Tolerability, and Pharmacokinetics of a Single Suspension Injection of Investigational Capsid Inhibitors Compared to Placebo in Healthy Adults (clinicaltrials.gov) - P1 | N=160 | Recruiting | Sponsor: ViiV Healthcare | Not yet recruiting ➔ Recruiting

Enrollment open • Human Immunodeficiency Virus • Infectious Disease

CINNAMON: Proof of Concept Treatment Study of Orally Administered VH4004280 or VH4011499 in HIV-1 Infected Adults (clinicaltrials.gov) - P2a | N=42 | Not yet recruiting | Sponsor: ViiV Healthcare

Monotherapy • New P2a trial • Human Immunodeficiency Virus • Infectious Disease • CD4

First-Time-in-Human (FTIH) Study to Evaluate the Safety, Tolerability and Pharmacokinetics (PK) of VH4011499 in Healthy Participants (clinicaltrials.gov) - P1 | N=73 | Completed | Sponsor: ViiV Healthcare | N=51 ➔ 73

Enrollment change • Human Immunodeficiency Virus • Infectious Disease

First-Time-in-Human (FTIH) Study to Evaluate the Safety, Tolerability and Pharmacokinetics (PK) of VH4011499 in Healthy Participants (clinicaltrials.gov) - P1 | N=51 | Completed | Sponsor: ViiV Healthcare | Recruiting ➔ Completed | N=90 ➔ 51

Enrollment change • Trial completion • Human Immunodeficiency Virus • Infectious Disease

First-Time-in-Human (FTIH) Study to Evaluate the Safety, Tolerability and Pharmacokinetics (PK) of VH4011499 in Healthy Participants (clinicaltrials.gov) - P1 | N=72 | Recruiting | Sponsor: ViiV Healthcare | Not yet recruiting ➔ Recruiting

Enrollment open • Human Immunodeficiency Virus • Infectious Disease

First-Time-in-Human (FTIH) Study to Evaluate the Safety, Tolerability and Pharmacokinetics (PK) of VH4011499 in Healthy Participants (clinicaltrials.gov) - P1 | N=72 | Not yet recruiting | Sponsor: ViiV Healthcare

New P1 trial • Human Immunodeficiency Virus • Infectious Disease