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Why Is Rapamycin Not a Rapalog?

Ajla Hodzic Kuerec1,2, Andrea B Maier3,4,5

  • 1Healthy Longevity Translational Research Program, Yong Loo Lin School of Medicine, National University of Singapore, Singapore, Singapore, dr.ajlahodzic@gmail.com.

Gerontology
|January 8, 2023
PubMed

Insights

Rapamycin, an FDA-approved immunosuppressant, is a promising drug for targeting aging. Its analogs, known as rapalogs, were developed to enhance its pharmacological properties like bioavailability and half-life.

Area of Science:

  • Gerontology and Pharmacology
  • Drug Development and Molecular Biology

Background:

  • Rapamycin (sirolimus) is an FDA-approved immunosuppressive drug with potential anti-aging applications.
  • Rapamycin and its analogs inhibit the mammalian target of rapamycin (mTOR) kinase.

Purpose of the Study:

  • To describe rapamycin and its analogs (rapalogs).
  • To highlight the development of rapalogs for improved pharmacological properties.

Main Methods:

  • Chemical structure comparison of rapamycin and its analogs.
  • Pharmacological property evaluation (bioavailability, half-life).

Main Results:

  • Rapamycin analogs share a similar chemical structure, differing at carbon-40.
  • Rapalogs were engineered to overcome limitations of rapamycin, such as poor oral bioavailability and short half-life.

Conclusions:

  • Rapalogs represent an advancement over rapamycin for therapeutic applications.
  • Understanding the structural and pharmacological differences is key to rapamycin analog development.
Keywords:
AgingMammalian target of rapamycin inhibitorsSirolimus

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