Selective optimization of side activities: the SOSA approach

Area of Science:

• Drug Discovery and Medicinal Chemistry
• Pharmacology
• Biotechnology

Background:

• High-Throughput Screening (HTS) is a common but resource-intensive method for identifying drug candidates.
• Existing drug molecules with confirmed human efficacy, bioavailability, and safety offer a valuable starting point for new therapeutic applications.

Purpose of the Study:

• To introduce and evaluate the Selective Optimization of Side Activities (SOSA) approach as a more efficient alternative to HTS.
• To demonstrate the potential of SOSA in generating novel, safe, and patentable drug analogues.

Main Methods:

• Utilizing a limited set of highly diverse drug molecules with pre-established safety and efficacy profiles.
• Employing traditional medicinal chemistry and parallel synthesis techniques.
• Modifying 'side activities' to become 'main activities' while reducing or eliminating original 'main activities'.

Main Results:

• The SOSA approach facilitates the transformation of secondary biological activities into primary therapeutic targets.
• This strategy leverages existing knowledge of drug safety and bioavailability.
• Successful generation of novel analogues with desired therapeutic effects.

Conclusions:

• The SOSA approach presents a strategic advantage over HTS for discovering new biological activities.
• SOSA increases the probability of developing safe, bioavailable, original, and patentable drug analogues.
• This method optimizes the drug discovery pipeline by building upon established drug profiles.