TPT-004 is a highly potent, selective tryptophan hydroxylase (TPH) with IC50 of 77 nM and 16 nM for TPH1 and TPH2, respectively.
TPT-004 displays no relevant impact at 20 μM on the function of the LAT1 transporter involved in the transport of tryptophan, phenylalanine, leucine, and histidine to the brain.
TPT-004 reduced the intracellular serotonin levels with IC50 of 0.952 uM in serotonergic BON cells, a human carcinoid cell line known to express TPH1.
TPT-004 showed efficacy in preclinical models of peripheral serotonin attenuation and colorectal tumor growth.
