It is known that an abnormal activation of the mitogen-activated protein kinase (MAPK) pathway is involved in tumor formation and progression, where MEK1 and MEK2 are the key proteins involved in this pathway. At the ongoing ASCO meeting in Chicago, Pasithea Therapeutics Corp. presented data on PAS-004, a macrocyclic MEK inhibitor for the potential treatment of cancer.
Meliora Therapeutics Inc. has patented cyclin-dependent kinase 11 (CDK11) inhibitors and apoptosis inducers reported to be useful for the treatment of breast cancer and melanoma.
Rakovina Therapeutics Inc. has described dual NAD+ ADP-ribosyltransferase (poly(ADP-ribose) polymerase; PARP) and histone deacetylase (HDAC) inhibitors reported to be useful for the treatment of Ewing sarcoma.
Bristol Myers Squibb Co. has identified proteolysis targeting chimera (PROTAC) compounds comprising a E3 ubiquitin ligase-binding moiety coupled to a proto-oncogene tyrosine-protein kinase receptor Ret (RET; CDHF12; PTC) targeting moiety through a linker reported to be useful for the treatment of cancer.
Almac Discovery Ltd. has nominated a new preclinical candidate molecule, ALM-401, a first-in-class bispecific antibody-drug conjugate (ADC) targeting EGFR/ROR1. It is being developed for the treatment of refractory lung cancer characterized by dual expression of ROR1 and EGFR.
Actym Therapeutics Inc. has obtained IND clearance from the FDA to begin a phase I trial of ACTM-838. The first-in-human study will enroll patients in the U.S. and Australia with advanced solid tumors who have failed prior lines of therapy and have no clinically beneficial treatment options.
Germline variants that did not affect gene function nevertheless affected multiple aspects of breast cancer risk, via their visibility to the immune system and its reactions. Perhaps most surprisingly, the same genetic constellations that were protective at the very earliest stage of breast cancer, stage 0 or ductal carcinoma in situ, were associated with worse outcomes once a tumor had become invasive.
Biosplice Therapeutics Inc. has disclosed dual-specificity tyrosine-(Y)-phosphorylation regulated kinase 1A (DYRK1A) inhibitors reported to be useful for the treatment of cancer, diabetes and Alzheimer’s disease.
KRAS is a GTPase that switches from an active GTP-bound conformation and an inactive GDP-bound conformation. Recently, several covalent KRAS G12C inhibitors that stick the protein in its GDP-bound inactive state have reached the clinic. However, the clinical benefit to date is limited and there is a need for next-generation compounds with better target engagement.
Full-Life Technologies Ltd. has received IND clearance by the FDA, allowing it to conduct clinical trials of 225Ac-FL-020, its PSMA-targeted radiopharmaceutical for the treatment of metastatic castration-resistant prostate cancer.
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