TTI-101 is an orally bioavailable, small-molecule inhibitor of signal transducer and activator of transcription 3 (STAT3), a transcription factor whose upregulation and activation governs many hallmarks of cancer, inflammation, and fibrosis. TTI-101 is well tolerated and has clinical activity in a first-in-man Phase 1 study in patients with advanced solid tumors. Preclinically, TTI-101 has demonstrated an excellent pharmacokinetic profile, potency in attenuating pY605-STAT3 phosphorylation, and efficacy in inhibiting tumor growth in xenograft and syngeneic tumor model.
TTI-102 is a next generation orally bioavailable, small molecule STAT3 inhibitor that is structurally related to, yet chemically distinct from TTI-101. TTI-102 has demonstrated key characteristics for clinical use including tolerability, bioavailability, and potency in preclinical studies.