MK-1088 / Merck (MSD) - LARVOL DELTA

Discovery of MK-1088 as a Potent A2A/A2B Adenosine Receptor Dual-Antagonist for Cancer Immunotherapy. (PubMed, J Med Chem) - "Simultaneous blockade of the downstream effects mediated by both receptor subtypes with a dual inhibitor has the potential to reverse adenosine-mediated suppression of tumor immune surveillance as either a single-agent treatment or in combination with other immunotherapy agents such as anti-PD-1/PD-L1 monoclonal antibodies. This publication describes the discovery and optimization of a novel series of potent and selective dual A2AR/A2BR antagonists, resulting in compound 46 (MK-1088) being identified for progression to human clinical studies."

Journal • Oncology • ADORA2A

A randomized phase 1 study of safety, tolerability, and pharmacokinetics of MK-1088, a novel dual adenosine receptor antagonist, in healthy adult participants. (PubMed, Invest New Drugs) - "A high-fat meal did not significantly affect pharmacokinetics at the 50-mg dose. MK-1088 was well tolerated and demonstrated dose-proportional pharmacokinetic properties that were not affected by a high-fat meal."

Journal • P1 data • PK/PD data

A Study of MK-1088 as Monotherapy and in Combination With Pembrolizumab in Participants With Advanced Solid Tumors (MK-1088-002) (clinicaltrials.gov) - P1/2 | N=27 | Terminated | Sponsor: Merck Sharp & Dohme LLC | N=80 ➔ 27 | Active, not recruiting ➔ Terminated; Business Reasons

Combination therapy • Enrollment change • Metastases • Monotherapy • Trial termination • Oncology • Prostate Cancer • Solid Tumor

A Study of MK-1088 as Monotherapy and in Combination With Pembrolizumab in Participants With Advanced Solid Tumors (MK-1088-002) (clinicaltrials.gov) - P1/2 | N=80 | Active, not recruiting | Sponsor: Merck Sharp & Dohme LLC | Trial completion date: May 2025 ➔ Sep 2023 | Trial primary completion date: May 2025 ➔ Sep 2023

Combination therapy • Metastases • Monotherapy • Trial completion date • Trial primary completion date • Oncology • Prostate Cancer • Solid Tumor

A Study of MK-1088 as Monotherapy and in Combination With Pembrolizumab in Participants With Advanced Solid Tumors (MK-1088-002) (clinicaltrials.gov) - P1/2 | N=80 | Active, not recruiting | Sponsor: Merck Sharp & Dohme LLC | Recruiting ➔ Active, not recruiting | Trial completion date: Nov 2025 ➔ May 2025 | Trial primary completion date: Nov 2025 ➔ May 2025

Combination therapy • Enrollment closed • Metastases • Monotherapy • Trial completion date • Trial primary completion date • Oncology • Prostate Cancer • Solid Tumor

A Study of MK-1088 as Monotherapy and in Combination With Pembrolizumab in Participants With Advanced Solid Tumors (MK-1088-002) (clinicaltrials.gov) - P1/2 | N=80 | Recruiting | Sponsor: Merck Sharp & Dohme LLC | Not yet recruiting ➔ Recruiting

Enrollment open • Oncology • Prostate Cancer • Solid Tumor

A Phase 1/Phase 2 Study to Evaluate the Safety and Tolerability of MK-1088 as Monotherapy/ single agent and in Combination with Pembrolizumab in Participants with Advanced Solid Tumors (clinicaltrialsregister.eu) - P1/2 | N=80 | Ongoing | Sponsor: Merck Sharp & Dohme Corp., a subsidiary of Merck & Co., Inc

Combination therapy • Monotherapy • New P1/2 trial • Oncology • Prostate Cancer • Solid Tumor • CD4

A Study of MK-1088 as Monotherapy and in Combination With Pembrolizumab in Participants With Advanced Solid Tumors (MK-1088-002) (clinicaltrials.gov) - P1/2 | N=80 | Not yet recruiting | Sponsor: Merck Sharp & Dohme LLC

Combination therapy • Monotherapy • New P1/2 trial • Oncology • Prostate Cancer • Solid Tumor