Mitapivat

Description: Mitapivat, previously also known as PKM2 activator 1020 is a PKM2 activator (pyruvate kinase activator) that has potential use for the treatment of pyruvate kinase deficiency. Mitapivat is a potent human R-type pyruvate kinase (PKR) inhibitor that also shows potency for mutant PKR including R510Q PKR, R532W PKR, T384W PKR etc. Pyruvate kinase type M2, which is expressed in multiple tumor cell types and plays a key role in aerobic glycolysis, has nonglycolytic functions and can regulate transcription and cell proliferation. Thus it has been reported that small molecule activators of pyruvate kinase isozyme M2 (PKM2) may suppress tumor formation but have an unknown effect on established tumors.

References: Oncotarget. 2017 Jul 26; 8(53):90959-90968; Technol Cancer Res Treat. 2018 Jan 1; 17:1533034617749418.