FULL SUPPLEMENT: DERMATOLOGIC DRUG DESIGN GOES RETRO

April 2022 | Volume 21 | Issue 4 | Department | S1188 | Copyright © April 2022


Published online March 31, 2022

Abstract
This supplement aims to provide a brief overview of retrometabolic drug design and a summary of the impact of the retrometabolic approach in other specialties. It highlights the use of retrometabolically designed drugs under investigation in dermatology, and specifically, hyperhidrosis.
In this supplement:

Retrometabolic Drug Delivery in Dermatology

A fundamental aspect of dermatologic diagnosis and treatment is our visibly ready access to the site of skin disease. Just as we can often render a diagnosis based on visual assessment of a lesion or rash, so can we often prescribe topical therapies that can be applied directly to the site of involvement. The complex and efficient stratum corneum generally facilitates localized treatment. It is usually possible to deliver therapeutically effective doses of active drugs in topical formulations such as: ointments, creams, lotions, gels, foams, and sprays that will act locally in the skin, being metabolized at the site of the disease and posing the potential for little or no resultant systemic exposure. Of course, there are no absolutes in medicine, and the inverse is also true: it is possible for some drugs to bypass the epidermal barrier to provide an action systemically.

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A Novel Drug Delivery Method: Retrometabolic Drug Design

Soft drugs, a class of retrometabolic drug design, contain a metabolically sensitive moiety that promotes rapid metabolism to inactive metabolites after exerting activity at its target site. The goal of soft drugs is to reduce systemic toxicity while enhancing local efficacy. Soft drugs have been approved for use in multiple medical specialties, such as the soft corticosteroid loteprednol etabonate for treatment of inflammatory ophthalmic disorders and soft beta-blocker derivatives for treatment of hypertensive emergencies in cardiology. Soft drugs have also found widespread use in the field of dermatology. In the setting of topical drug administration, soft drugs minimize the risk of systemic drug absorption and unwanted side effects.

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