tomivosertib

Tomivosertib is an orally bioavailable, highly selective small molecule inhibitor of mitogen‑activated protein kinase (MAPK)‑interacting serine/threonine-protein kinases 1 and 2 (MNK1 and MNK2). By inhibiting MNK1/2 activity, tomivosertib blocks phosphorylation of the eukaryotic translation initiation factor 4E (eIF4E), a key regulator of mRNA translation involved in tumor cell proliferation, angiogenesis, survival, and immune signaling. This mechanism disrupts oncogenic protein synthesis pathways in cancer cells. Tomivosertib has been investigated primarily as an antineoplastic agent for various solid tumors including non-small cell lung cancer (NSCLC), triple negative breast cancer (TNBC), diffuse large B cell lymphoma (DLBCL), colorectal cancer, liver cancer, prostate cancer, and acute myeloid leukemia. The drug was developed by eFFECTOR Therapeutics and has reached phase II clinical trials in several indications; however, development for frontline NSCLC was terminated after modest efficacy results[1][3][5][7].

Other names

6'-((6-Amino-4-pyrimidinyl)amino)-8'-methyl-2'H-spiro(cyclohexane-1,3'-imidazo(1,5-a)pyridine)-1',5'-dioneTomivosertib hydrochloride