FDA-approved drugs featuring macrocycles or medium-sized rings.

Area of Science:

• Medicinal Chemistry
• Organic Synthesis
• Drug Discovery

Background:

• Macrocycles possess unique structural and functional properties, enabling high affinity and selectivity for protein targets.
• These properties, combined with good bioavailability, make macrocycles valuable in drug discovery for various therapeutic areas.
• Over 60 macrocyclic drugs have been approved by the FDA since the 20th century.

Purpose of the Study:

• To review 17 Food and Drug Administration (FDA)-approved macrocyclic drugs from the past five years.
• To emphasize the significance and therapeutic impact of these macrocycles.
• To showcase innovative synthetic methodologies for macrocycle construction.

Main Methods:

• Literature review of FDA-approved macrocyclic drugs.
• Analysis of synthetic approaches for macrocycle development.
• Highlighting key features and therapeutic applications.

Main Results:

• Seventeen macrocyclic drugs approved by the FDA in the last five years were identified.
• These drugs demonstrate broad therapeutic applications, including infections, cancer, and neurological disorders.
• Innovative synthetic strategies have facilitated the development of these complex molecules.

Conclusions:

• Macrocycles represent a critical and expanding class of therapeutics.
• Recent advancements in synthetic chemistry are driving the discovery of novel macrocyclic drugs.
• The continued development of macrocyclic drugs holds significant promise for future medicine.