Drug intelligence / Profile preview

RA836

Development stage
Preclinical
Modality
Small Molecules
01

Overview

RA836 is a **potent small molecule inhibitor** of solute carrier family 6 member 19 (**SLC6A19**, also known as the neutral amino acid transporter B^0AT1) that has been investigated for its effects on the modulation of indoxyl sulfate (IDS) accumulation via simultaneous inhibition of SLC6A19 in the gastrointestinal tract and breast cancer resistance protein (**BCRP**, also known as ABCG2) in the kidney. RA836 elevates tissue and plasma levels of the uremic toxin IDS by increasing its production through tryptophan metabolism (SLC6A19 inhibition) and blocking its renal excretion (BCRP inhibition). The compound shows **no significant inhibition** of other kidney transporters such as organic anion transporter 1 (**OAT1**) or OAT3. Its primary potential indication has been the treatment of **phenylketonuria**, but SLC6A19 inhibitors also have implications in metabolic and renal disorders. Its use is cautioned due to risks of IDS accumulation, a known risk factor in cardiovascular and kidney disease[1][3].

02

Targets

SLC6A19 (Na+-dependent system B0 transporter)ABCG2 (ATP-binding cassette sub-family G member 2)

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