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FRα is a high-affinity receptor for folates with restricted expression in normal tissue and overexpression in many solid tumors (eg, ovarian and lung adenocarcinoma). Supporting the high demand of cancer cells for folate to increase metabolism and proliferation is its main function.1
AZD5335 is a FRalpha-targeting antibody-drug conjugate conjugated to topoisomerase 1 inhibitor (TOP1) payload with potential bystander antitumor activity. Upon internalization and trafficking to the lysosome, the TOP1i payload is released. Binds and traps topoisomerase 1 on DNA and eventually causes cell death.2
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deoxyribonucleic acid
folate receptor α
topoisomerase 1 inhibitor
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deoxyribonucleic acid
folate receptor α
topoisomerase 1 inhibitor