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Pimasertib is an orally bioavailable, highly selective small molecule inhibitor of mitogen‐activated protein kinases 1 and 2 (MEK1/2), key components of the MAPK/ERK signaling pathway. By selectively binding to and inhibiting MEK1 and MEK2, pimasertib prevents activation of downstream effector proteins and transcription factors, resulting in inhibition of growth factor-mediated cell signaling and tumor cell proliferation. It has demonstrated potent antitumor activity in preclinical models both as monotherapy and in combination with other agents. Pimasertib was developed for the treatment of various solid tumors but its clinical development has been discontinued for several indications[1][3][4][5][7].
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