A Phase 1/Phase 2 Study to Evaluate the Safety and Tolerability of MK-1088 as Monotherapy and in Combination With Pembrolizumab in Participants With Advanced Solid Tumors

The study will evaluate the safety, tolerability, and pharmacokinetics (PK) of MK-1088 in monotherapy and in combination with pembrolizumab in participants with advanced solid tumors who have not responded to conventional therapy. The effect of MK-1088 on tumor size will also be examined.

Start Date07 Jul 2022

Sponsor / Collaborator

Merck Sharp & Dohme Corp.

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01 Oct 2024·Investigational New Drugs

A randomized phase 1 study of safety, tolerability, and pharmacokinetics of MK-1088, a novel dual adenosine receptor antagonist, in healthy adult participants

Article

Author: Stoch, Aubrey ; Lemoine, Lieselotte ; Kim, Yeonil ; Deschamps, Kathleen ; Gupta, Pranav ; Rottey, Sylvie ; Matthews, Catherine Zhou ; Lai, Eseng ; Van Dyck, Kristien ; Chatterjee, Manash

AbstractThis phase 1 first-in-human study evaluated the safety, tolerability, and pharmacokinetics of MK-1088, a novel, small-molecule dual inhibitor of adenosine A2A and A2B receptors. Healthy adult participants were enrolled in two panels (n = 8 each) and randomly assigned to receive MK-1088 (n = 6) or placebo (n = 2) orally in each of five treatment periods. Participants in panel A received single ascending doses of MK-1088 at 1, 10, 50, and 150 mg or placebo in a fasted or fed (50 mg only) state. Participants in panel B received MK-1088 at 3, 25, 100, and 224 mg or placebo in a fasted state. Primary objectives were to evaluate safety, tolerability, and plasma pharmacokinetics following a single dose of MK-1088. The secondary objective was to evaluate the effects of a high-fat meal on pharmacokinetics. All participants (n = 16) completed the study (median age: 33 years [range: 20–43]; all were male). Treatment-related adverse events (AEs) occurred in 1 of 6 (17%), 4 of 6 (67%), 4 of 6 (67%), and 2 of 6 (33%) participants after receiving MK-1088 at 3, 25, 100, and 224 mg, respectively. No serious AEs or deaths due to any cause occurred. MK-1088 was rapidly absorbed after a single dose; half-life was ~ 11 h in the 100–224 mg dose range. The target concentration at 12 h (> 0.3 µM) was exceeded at the 50-mg dose level. MK-1088 plasma pharmacokinetics increased dose proportionately. 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.

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Indication	Highest Phase	Country/Location	Organization	Date
Advanced Malignant Solid Neoplasm	Phase 2	United States	Merck Sharp & Dohme Corp.	07 Jul 2022
Advanced Malignant Solid Neoplasm	Phase 2	Israel	Merck Sharp & Dohme Corp.	07 Jul 2022
Advanced Malignant Solid Neoplasm	Phase 2	Canada	Merck Sharp & Dohme Corp.	07 Jul 2022
Advanced Malignant Solid Neoplasm	Phase 2	Denmark	Merck Sharp & Dohme Corp.	07 Jul 2022
Advanced Malignant Solid Neoplasm	Phase 2	Switzerland	Merck Sharp & Dohme Corp.	07 Jul 2022

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT05394350 (MK-1088-002, CTgov)	Phase 1/2	Advanced Malignant Solid Neoplasm	27	MK-1088 (MK-1088 100 mg)	jfeewyrska(gpkndoddsj) = vboytwurxi ipzbptmnqy (wfohrkjtkj, qshhmhrfuk - vfsylddupx) View more	-	04 Oct 2024
				MK-1088 (MK-1088 200 mg)	jfeewyrska(gpkndoddsj) = fqthvktfun ipzbptmnqy (wfohrkjtkj, oeuzmwcpaa - byytxrspab) View more

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