Drug intelligence / Profile preview

alpha-methyl-L-tryptophan C-11

Development stage
Unknown
Lead developer
Takeda
Modality
Small Molecules, Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics
Administration
Intravenous
01

Overview

Alpha-methyl-L-tryptophan C-11 ([11C]AMT) is a radiopharmaceutical PET tracer designed to image and quantify regional serotonin synthesis and kynurenine pathway activity in the brain. As a synthetic analog of the essential amino acid L-tryptophan, it is transported across the blood-brain barrier via the large neutral amino acid transporter (LAT1). Once in the brain, it serves as a substrate for tryptophan hydroxylase (TPH), the rate-limiting enzyme in serotonin production. Unlike endogenous tryptophan, [11C]AMT is not incorporated into proteins and its metabolites are trapped within the tissue, allowing for the measurement of the serotonin synthesis rate. Additionally, [11C]AMT is a substrate for indoleamine 2,3-dioxygenase (IDO), making it a valuable tool for imaging the kynurenine pathway, which is often upregulated in neuroinflammatory conditions, certain brain tumors (gliomas), and epileptogenic tubers in patients with Tuberous Sclerosis Complex (TSC).

Other names
alpha-methyl-L-tryptophan (11C)11C-alpha-methyl-L-tryptophanCarbon-11 alpha-methyl-L-tryptophanCarbon11 alpha-methyl-L-tryptophanCarbon 11 alpha-methyl-L-tryptophan
02

Targets

IDO1 (Indoleamine 2,3-dioxygenase 1)TPH2 (Tryptophan hydroxylase 2)SLC7A5 (Large neutral amino acid transporter small subunit 1)TPH1 (Tryptophan 5-hydroxylase 1)

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