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Luminespib (AUY922) is a second-generation heat shock protein 90 (HSP90) inhibitor with demonstrated activity in non-small cell lung cancer (NSCLC). Pemetrexed is an antifolate chemotherapy agent. The combination of luminespib and pemetrexed has been investigated for the treatment of previously treated metastatic non-squamous NSCLC. Luminespib reduces levels of dihydrofolate reductase (DHFR), a key enzymatic target of pemetrexed, which may enhance the therapeutic effect. Clinical studies have shown that this combination demonstrates clinical activity, but tolerability is limited by ocular toxicity[1].
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