Loading
How well a drug crosses from the blood into the brain, where most cancer drugs are kept out by the blood-brain barrier. Brain-penetrant pills can treat and prevent brain metastases; those that are not leave the brain as a sanctuary where the cancer regrows.
Third-generation EGFR (osimertinib) and ALK (alectinib, lorlatinib) inhibitors were designed for CNS penetration and cut brain progression dramatically compared with earlier drugs; tucatinib, and unexpectedly T-DXd, are active against HER2-positive brain metastases; temozolomide, lomustine and vorasidenib are brain-penetrant by design. Penetration is measured as unbound brain-to-plasma ratio (Kp,uu) or CSF concentration and is limited by efflux pumps (P-glycoprotein, BCRP). Intracranial response rates and CNS progression-free survival are now standard secondary endpoints in lung and breast cancer trials, and intrathecal or intraventricular delivery bypasses the barrier for leptomeningeal disease.
Showing the molecule this term concerns: Osimertinib.
Shares Tucatinib, Osimertinib, Trastuzumab deruxtecan.
Shares Intrathecal therapy (lumbar puncture, Ommaya reservoir), CNS prophylaxis in aggressive B-cell lymphoma, and the evidence against it, Primary CNS lymphoma, Diffuse large B-cell lymphoma.
Shares Intrathecal therapy (lumbar puncture, Ommaya reservoir), Brain metastases (intracranial disease).
Shares Tyrosine kinase inhibitor (TKI), Brain metastases (intracranial disease), Osimertinib.
Shares Leptomeningeal disease, Brain metastases (intracranial disease), Trastuzumab deruxtecan.
Shares Tucatinib, Trastuzumab deruxtecan.
Shares Temozolomide, Trastuzumab deruxtecan.
Shares Brain metastases (intracranial disease), Osimertinib.