MK-8242 / Merck (MSD) - LARVOL DELTA

Small-molecule MDM2/X inhibitors and PROTAC degraders for cancer therapy: advances and perspectives. (PubMed, Acta Pharm Sin B) - "Numerous small-molecule MDM2 inhibitors have been reported since the release of the structure of the MDM2-P53 interaction in 1996, SAR405838, NVP-CGM097, MK-8242, RG7112, RG7388, DS-3032b, and AMG232 currently undergo clinical evaluation for cancer therapy. This review is intended to provide a comprehensive and updated overview of MDM2 inhibitors and proteolysis targeting chimera (PROTAC) degraders with a particular focus on how these inhibitors or degraders are identified from starting points, strategies employed, structure-activity relationship (SAR) studies, binding modes or co-crystal structures, biochemical data, mechanistic studies, and preclinical/clinical studies. Moreover, we briefly discuss the challenges of designing MDM2/X inhibitors for cancer therapy such as dual MDM2/X inhibition, acquired resistance and toxicity of P53 activation as well as future directions."

Journal • Review • Oncology • Targeted Protein Degradation

Study of Safety and Pharmacokinetics of MK-8242 in Participants With Advanced Solid Tumors (P07650) (clinicaltrials.gov) - P1; N=47; Completed; Sponsor: Merck Sharp & Dohme Corp.; Active, not recruiting -> Completed ; N=86 -> 47

Enrollment change • Trial completion • Biosimilar • Oncology

MK-8242 Is Active in Patients with p53 Wild-Type Advanced Solid Tumors. (PubMed) - Cancer Discov - "The MDM2 inhibitor MK-8242 is tolerable in patients with liposarcoma and other advanced solid tumors."

Journal • Biosimilar • Oncology • Sarcoma