372
ANTINEOPLASTIC
IMMUNOSUPPRESSIVE ANTIMETABOLITES
ANTIRHEUMATIC AGENTS
AZATHIOPRINE IS METABOLIZED TO 6-MERCAPTOPURINE (6-MP) AND THEN BY HYPOXANTHINE-GUANINE PHOSPHORIBOSYLTRANSFERASE (HGPRT) AND DIVERSES KINASES WHICH LEAD TO THE INCORPORATION OF 6-THIOGUANINE NUCLEOTIDES (6-TGN) INTO DNA
ORAL INJECTION
ATC code
L04AX01
Tmax 1.5 HOUR
PPB 30 PERCENT
INSOLUBLE IN WATER
TARGET DNA
Unknown
Formula:
C9H7N7O2S
Calculated chemical properties:
NB_atoms 19
XLogP 0
PSA 103.414
NB_HD 1
NB_HA 8
fsp3 0.11
Lipinski(0=no;1=yes) 1
NDA 071056 (pdf not found) INN (AZATHIOPRINE SODIUM) AZATHIOPRINE (QUAD PHARMS) APPROVAL= - YEAR= 0 DISCONTINUED
NDA 016324 (label) INN (AZATHIOPRINE) IMURAN (LEGACY) APPROVAL= AP YEAR= 1968 NEWMOLECULARENTITY
NDA 017391 (label) INN (AZATHIOPRINE SODIUM) IMURAN (CASPER PHARMA LLC) APPROVAL= AP YEAR= 1974 DISCONTINUED
NDA 074419 (pdf not found) INN (AZATHIOPRINE SODIUM) AZATHIOPRINE SODIUM (HIKMA) APPROVAL= AP YEAR= 1995
NDA 074069 (pdf not found) INN (AZATHIOPRINE) AZATHIOPRINE (AMNEAL) APPROVAL= AP YEAR= 1996
NDA 075252 (pdf not found) INN (AZATHIOPRINE) AZASAN (AAIPHARMA LLC) APPROVAL= AP YEAR= 1999
NDA 075568 (pdf not found) INN (AZATHIOPRINE) AZATHIOPRINE (RISING) APPROVAL= AP YEAR= 1999
NDA 077621 (pdf not found) INN (AZATHIOPRINE) AZATHIOPRINE (ZYDUS PHARMS USA) APPROVAL= AP YEAR= 2007
NDA 208687 (pdf not found) INN (AZATHIOPRINE) AZATHIOPRINE (ALKEM LABS LTD) APPROVAL= AP YEAR= 2020
139
ANTINEOPLASTIC
TREATMENT OF ACUTE LYMPHOBLASTIC LEUKAEMIA (ALL) (DRUG FOR RARE DISEASE IN EUROPE)
ANTIMETABOLITES IMMUNOSUPPRESSIVE AGENTS
NUCLEIC ACID SYNTHESIS INHIBITORS
PURINE ANALOGUES
MODIFIED BY HYPOXANTHINE-GUANINE PHOSPHORIBOSYLTRANSFERASE (HGPRT) TO TIMP (THIOINOSINE MONOPHOSPHATE) AND THEN DIVERSES KINASES (INOSINE MONOPHOSPHATE DEHYDROGENASE, GUANOSINE MONOPHOSPHATE SYNTHETASE AND KINASES) WHICH LEAD TO THE INCORPORATION OF 6-THIOGUANINE NUCLEOTIDES (6-TGN) INTO DNA
ORAL
ATC code
L01BB02
VD 65 LITER (65 KILOGRAM)
Cl 58.5 LITER / HOUR (65 KILOGRAM)
PPB 15 PERCENT
t1/2 1 HOUR
TARGET HYPOXANTHINE-GUANINE PHOSPHORIBOSYLTRANSFERASE (HGPRT)
Amidophosphoribosyltransferase UNIPROT Q06203 PPAT
Formula:
C5H4N4S
Calculated chemical properties:
NB_atoms 10
XLogP 1.02
PSA 48.428
NB_HD 2
NB_HA 4
fsp3 0.00
Lipinski(0=no;1=yes) 1
NDA 009053 (label) INN (MERCAPTOPURINE) PURINETHOL (STASON PHARMS) APPROVAL= AP YEAR= 1953
NDA 040461 (pdf not found) INN (MERCAPTOPURINE) MERCAPTOPURINE (DR REDDYS LABS SA) APPROVAL= AP YEAR= 2004
NDA 040528 (pdf not found) INN (MERCAPTOPURINE) MERCAPTOPURINE (HIKMA) APPROVAL= AP YEAR= 2004
NDA 040594 (pdf not found) INN (MERCAPTOPURINE) MERCAPTOPURINE (MYLAN) APPROVAL= AP YEAR= 2005 DISCONTINUED
NDA 205919 (label) INN (MERCAPTOPURINE) PURIXAN (NOVA LABS LTD) APPROVAL= AP YEAR= 2014
NDA 216418 (pdf not found) INN (MERCAPTOPURINE) MERCAPTOPURINE (HIKMA) APPROVAL= AP YEAR= 2025