enbezotinib (TPX-0046)

P1/2, N=41, Terminated, Turning Point Therapeutics, Inc. | Trial completion date: Nov 2023 --> May 2023 | Active, not recruiting --> Terminated; Adverse change in the risk/benefit.

Thus, the novel highly potent and RET-specific inhibitors selpercatinib and pralsetinib have been accelerated for approval by the Food and Drug Administration (FDA), and clinical trials of TPX-0046 and zetletinib are underway. It is well tolerated and a potential therapeutic for RET-altered cancers. Thus, we will focus on current state-of-the-art therapeutics with these novel RET inhibitors and show their efficacy and safety in therapy.

P1/2, N=462, Active, not recruiting, Turning Point Therapeutics, Inc. | Recruiting --> Active, not recruiting

P1/2, N=462, Recruiting, Turning Point Therapeutics, Inc. | Trial completion date: Mar 2025 --> Nov 2026 | Trial primary completion date: May 2024 --> Dec 2025

Selective RET inhibitors (selpercatinib/pralsetinib) are active in patients with these cancers; unfortunately, resistance often occurs. TPX-0046 is a unique next-generation RET inhibitor that possesses potent in vitro and in vivo activity against a diverse range of RET alterations, including SFM-mediated resistance. A phase 1/2 trial for RET inhibitor-resistant and naïve RET-driven cancers is on-going (NCT04161391). Research Funding: Turning Point Therapeutics