Urothelial cancer, locally advanced or metastatic

Antineoplastic Agent, Anti-Nectin-4
Enfortumab vedotin is an antibody drug conjugate (ADC) directed at Nectin-4 (an adhesion protein located on cell surfaces). It contains an IgG1 anti-Nectin-4 antibody conjugated to a microtubule-disrupting agent, monomethyl auristatin E (MMAE). MMAE is attached to the antibody via a protease cleavable linker. The ADC binds to Nectin-4 expressing cells to form a complex which is internalized within the cell. Released MMAE binds to the tubules and disrupts the cellular microtubule network, inducing cell cycle arrest and apoptosis of Nectin-4 expressing cells

1.Distribution: Vdss: Antibody drug conjugate (ADC): 12.8 L.
2.Protein binding: Unconjugated monomethyl auristatin E (MMAE): 68% to 82%.
3.Metabolism: Enfortumab vedotin is expected to undergo catabolism to small peptides, amino acids, unconjugated MMAE, and unconjugated MMAE-related catabolites. Unconjugated MMAE is released from the ADC via proteolytic cleavage and is primarily metabolized by CYP3A4.
4.Half-life elimination: ADC: 3.6 days; MMAE: 2.6 days.
5.Time to peak: ADC: at the end of the infusion; unconjugated MMAE: At ~2 days after a dose.
6.Excretion: Unconjugated MMAE: Feces: 17%; urine: 6%; primarily as unchanged form

Hypersensitivity to enfortumab vedotin or any component of the formulation.

Fetal risk cannot be ruled out.
Available evidence is inconclusive or inadequate for determining fetal risk when used in pregnant women.

Based on the mechanism of action and data from animal reproduction studies, in utero exposure to enfortumab vedotin may cause fetal harm.

fatigue、hair loss、decreased appetite、peripheral neuropathy、neutropenia、anemia、papular rash

Mild impairment (total bilirubin 1 to 1.5 times ULN and any AST, or total bilirubin ULN and AST > ULN): There are no dosage adjustments provided in the manufacturer’s labeling