selpercatinib + dabigatran

The combination of two pharmaceutical agents: selpercatinib, an oral, small molecule kinase inhibitor that selectively inhibits the rearranged during transfection (RET) receptor tyrosine kinase, and dabigatran, an oral direct thrombin (factor IIa) inhibitor used as an anticoagulant. Selpercatinib is primarily indicated for treatment of RET fusion-positive cancers such as non-small cell lung cancer (NSCLC) and certain thyroid cancers. Dabigatran is prescribed for prevention of stroke and systemic embolism in patients with non-valvular atrial fibrillation, and for treatment and prevention of deep vein thrombosis and pulmonary embolism. When used together, selpercatinib increases plasma concentrations of dabigatran due to its inhibition of P-glycoprotein (P-gp), the main transporter responsible for dabigatran absorption and disposition. This leads to an approximate 1.4-fold increase in dabigatran exposure, raising the risk of bleeding. To mitigate this, administration of dabigatran is recommended at least 2 hours before selpercatinib in the fasted state[1][2].