Drug intelligence / Profile preview

TAFA-93

Development stage
Discontinued
Lead developer
Aurinia
Modality
Nucleic Acid-Directed Small Molecules → Small Molecules, Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

TAFA-93 is a novel small molecule prodrug of the mTOR inhibitor rapamycin (also known as sirolimus). It was developed as an oral immunosuppressive agent for the prevention of organ transplant rejection. As a prodrug, it is metabolized in the body to release rapamycin, which inhibits the mechanistic target of rapamycin (mTOR), a serine/threonine-protein kinase involved in cell growth and proliferation. mTOR inhibitors are used clinically to prevent organ rejection after transplantation and have applications in autoimmune diseases and oncology. TAFA-93 was investigated primarily for use in transplant rejection but development was discontinued after Phase 1 clinical trials[1][2][3][4][9].

02

Targets

Mechanistic target of rapamycin complex 1

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