MLE-301

MLE-301 is a **potent, selective, and reversible antagonist of the human neurokinin 3 receptor (NK3R)**, developed for the treatment of vasomotor symptoms (VMS)—such as hot flashes and night sweats—in menopausal women. It acts by inhibiting NK3R signaling on KNDy (kisspeptin/neurokinin B/dynorphin) neurons, which are key in the pathogenesis of VMS, thereby aiming to reduce the frequency and severity of these symptoms. The drug was originally developed by Roche and later taken up by Millendo Therapeutics. MLE-301 was investigated in clinical trials, including a Phase 1 study assessing safety, tolerability, pharmacokinetics, and preliminary efficacy. **Development has been discontinued for its primary indication of VMS in menopausal women**[1][2][4][7][9][10].