MK-1084 News - LARVOL Sigma

|||||||||| MK-1084 / Merck (MSD), Otsuka
Journal: Discovery of MK-1084: An Orally Bioavailable and Low-Dose KRASG12C Inhibitor. (Pubmed Central) - Jun 26, 2024
P1
Herein, we disclose our journey toward the discovery of MK-1084, an orally bioavailable and low-dose KRASG12C covalent inhibitor currently in phase I clinical trials (NCT05067283). We leveraged structure-based drug design to identify a macrocyclic core structure, and hypothesis-driven optimization of biopharmaceutical properties to further improve metabolic stability and tolerability.

||||||||||  MK-1084 / Merck (MSD), Otsuka
Enrollment change, Combination therapy, Monotherapy, Metastases:  A Study of MK-1084 in KRAS Mutant Advanced Solid Tumors (MK-1084-001) (clinicaltrials.gov) -  Apr 17, 2024
P1, N=830, Recruiting,  Sponsor: Merck Sharp & Dohme LLC
We leveraged structure-based drug design to identify a macrocyclic core structure, and hypothesis-driven optimization of biopharmaceutical properties to further improve metabolic stability and tolerability. N=450 --> 830

||||||||||  Keytruda (pembrolizumab) / Merck (MSD), MK-1084 / Merck (MSD), Otsuka
New P3 trial, Combination therapy, Tumor proportion score, IO biomarker, Metastases:  A Study of MK-1084 Plus Pembrolizumab (MK-3475) in Participants With KRAS G12C Mutant, Metastatic Non-small Cell Lung Cancer (NSCLC) With Programmed Cell Death Ligand 1 (PD-L1) Tumor Proportion Score (TPS) ?50% (MK-1084-004) (clinicaltrials.gov) -  Apr 2, 2024
P3, N=600, Not yet recruiting,  Sponsor: Merck Sharp & Dohme LLC

|||||||||| MK-1084 / Merck (MSD), Otsuka
A phase 1, open-label, multicenter study evaluating MK-1084 as monotherapy and in combination with other therapies in patients with KRAS G12C mutant advanced solid tumors. (Level 1, West Hall; Poster Bd # N20) - Dec 6, 2023 - Abstract #ASCOGI2024ASCO_GI_645;
P1
N=450 --> 830 ESMO 2023; Abs 3156) indicated antitumor activity in pts with solid tumors receiving oral MK-1084 monotherapy QD or BID (25 to 800 mg total daily; arm 1) and pts with previously untreated non

|||||||||| MK-1084 / Merck (MSD)
Discovery of MK-1084, a low dose selective clinical stage KRAS G12C inhibitor. (LEVEL 2, EXHIBIT HALL D) - Sep 16, 2023 - Abstract #AACRNCIEORTC2023AACR_NCI_EORTC_397;

|||||||||| Keytruda (pembrolizumab) / Merck (MSD), MK-1084 / Merck (MSD)
Safety and preliminary efficacy of the KRAS G12C Inhibitor MK-1084 in solid tumors and in combination with pembrolizumab in NSCLC () - Jul 27, 2023 - Abstract #ESMO2023ESMO_2236;
P1
Conclusions MK-1084 as monotherapy and in combination with pembro showed manageable safety and preliminary antitumor activity in pts with previously treated solid malignancies and previously untreated NSCLC whose tumors harbored KRAS G12C mutations. Study is ongoing; updated data will be presented.

||||||||||  MK-1084 / Merck (MSD), Otsuka
Enrollment change, Trial completion date, Trial primary completion date, Combination therapy, Monotherapy, Metastases:  A Study of MK-1084 in KRAS Mutant Advanced Solid Tumors (MK-1084-001) (clinicaltrials.gov) -  Apr 27, 2023
P1, N=450, Recruiting,  Sponsor: Merck Sharp & Dohme LLC
Study is ongoing; updated data will be presented. N=264 --> 450 | Trial completion date: Feb 2026 --> Aug 2026 | Trial primary completion date: Feb 2026 --> Aug 2026

||||||||||  MK-1084 / Merck (MSD), Otsuka
Enrollment change, Combination therapy, Monotherapy, Metastases:  A Study of MK-1084 in KRAS Mutant Advanced Solid Tumors (MK-1084-001) (clinicaltrials.gov) -  Sep 19, 2022
P1, N=264, Recruiting,  Sponsor: Merck Sharp & Dohme LLC
N=264 --> 450 | Trial completion date: Feb 2026 --> Aug 2026 | Trial primary completion date: Feb 2026 --> Aug 2026 N=185 --> 264

||||||||||  MK-1084 / Merck (MSD), Otsuka
Enrollment open, Combination therapy, Monotherapy, Metastases:  A Study of MK-1084 in KRAS Mutant Advanced Solid Tumors (MK-1084-001) (clinicaltrials.gov) -  Dec 14, 2021
P1, N=185, Recruiting,  Sponsor: Merck Sharp & Dohme Corp.
N=185 --> 264 Not yet recruiting --> Recruiting

||||||||||  MK-1084 / Merck (MSD), Otsuka
New P1 trial, Combination therapy, Monotherapy, Metastases:  A Study of MK-1084 in KRAS Mutant Advanced Solid Tumors (MK-1084-001) (clinicaltrials.gov) -  Oct 5, 2021
P1, N=185, Not yet recruiting,  Sponsor: Merck Sharp & Dohme Corp.



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