Tioguanine

Tioguanine

Clinical data
Routes of administration	oral
ATC code	L01BB03 (WHO)
Pharmacokinetic data
Bioavailability	30% (range 14% to 46%)
Metabolism	Intracellular
Elimination half-life	80 minutes (range 25-240 minutes)
Identifiers
IUPAC name 2-amino-7H-purine-6-thiol
CAS Number	154-42-7
PubChem CID	2723601
DrugBank	APRD00290
E number	{{#property:P628}}
ECHA InfoCard	{{#property:P2566}}
Chemical and physical data
Formula	C5H5N5S
Molar mass	167.193 g/mol

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Evidence Based Medicine
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Clinical Trials
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Definitions
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Experimental / Informatics
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Overview

Tioguanine (INN), formerly Thioguanine (BAN), is a drug that is used in the treatment of cancer. It belongs to the family of drugs called antimetabolites. It is a guanine analog. Its principal use is in acute leukaemias and chronic myeloid leukaemia.

Pharmacology

As a guanine analogue, it is transformed inside the cell into to 6-thioguanilyic acid (TGMP) which, by pseudofeedback interference with purine biosynthesis, interferes with the synthesis of guanine nucleotides. Some of its activity may also be due to the incorporation of thioguanine nucleotides into both RNA and DNA, but the end result is inducing cell cycle arrest and apoptosis. It is metabolized by via methylation by thiopurine methyltransferase.

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