The Takeda brain-penetrant M1R positive allosteric modulator (PAM), TAK-071, was optimized for lower cooperativity (α) with the native ligand to theoretically reduce the side effect of diarrhea from M1R activation. In animal models, higher cooperativity on M1R was associated with diarrhea, while lower cooperativity led to a wider margin. In [...]
< 1 minute read
Dec. 16, 2021
TAK-071: a Brain-Penetrant M1R Positive Allosteric Modulator (PAM)
TAK-071
low α- M1R positive allosteric modulator 7.5 mg+ PO QD in Ph. II for Parkinson’s from eval. of M1R PAMs w/ low cooperativity British Journal of Clinical Pharmacology Takeda Pharmaceutical, Cambridge, USA
Loading...
