Effects of Vinblastine and Its Metabolites on Nausea and Alopecia Associated Receptors
December 2018
TLDR Vinblastine and its metabolites may cause nausea and hair loss by binding to specific receptors and could lead to better chemotherapy drugs with fewer side effects.
In 2018, Caroline Manto Chagas' Masters thesis investigated the effects of vinblastine (VLB) and its 35 known metabolites on nausea and alopecia associated receptors using molecular docking simulations. The study found that VLB and its metabolites have binding affinities mainly for the muscarinic receptors M₁, M₄, and M₅, which play significant roles in the onset of nausea during chemotherapy. Additionally, VLB metabolites showed binding affinities for alopecia associated receptors such as vitamin D (VDR), androgen, smoothened, and MDM2, which can trigger hair follicle death following cancer treatment. The study suggested that understanding which and how the metabolites of VLB are involved with off-target receptors of nausea and alopecia could help eliminate or lessen adverse drug reactions during chemotherapy. This could be achieved through modifications on the chemical structure of VLB and advances in drug discovery and medicinal chemistry fields.