AUM601
Pan-specific kinase inhibitor
AUM601 is a highly selective, orally administered, which inhibits not only pan-TRK(TRKA, TRKB, and TRKC), but also resistance mutations of TRKs, by blocking the activity of tyrosine kinases, suggesting a more potent anti-tumor activity. It also shows excellent PK profile with higher distribution in tissue than blood, and the lowest distribution in brain suggesting low CNS toxicity. It has highly favorable safety profile and superior AUC, Cmax and tumor concentration resulting in enhanced target engagement and patient convenience.
MECHANISM OF ACTION
The neurotrophin tyrosine receptor kinase (NTRK) family composed of three members, TRKA, TRKB, and TRKC. These Tropomyosin receptor kinase (TRK) proteins are single-pass transmembrane proteins, expressed in the nervous system and in many non-neuronal tissue types. It has been observed that the occurrence of NTRK gene fusion between NTRK1, 2, or 3 and various unrelated gene partners, represents the genomic alteration with oncogenic potential, which has been observed in a wide range of human tumor types in comparison to oncogenic mechanisms.
