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Off-Target Receptor Activation

Meaning

Off-Target Receptor Activation describes the undesirable pharmacological phenomenon where a therapeutic agent, such as a synthetic hormone or drug, binds to and activates a receptor other than its intended primary target. This lack of precise selectivity can trigger unintended biological cascades, leading to a spectrum of adverse effects or side effects that compromise the drug’s safety profile. In the realm of hormonal therapy, this is a critical consideration, as it can result in cross-activation of receptors for related steroids, producing unwanted androgenic or glucocorticoid effects.