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Prodrugs

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Definition: A compound that, on administration, must undergo chemical conversion by metabolic processes before becoming the pharmacologically active drug for which it is a prodrug.  "a cpd that on admin must undergo chem conversion by metab processes before becoming the pharmacologically active drug for which it is a prodrug"; D25-26 qualif; coord IM with specific drug (IM)    Other names Drug Precursors; Pro Drugs; Precursors, Drug; Pro-Drugs
 
SubstanceCAS Registry & nameCategoriesSourceDrugs*
IDX184  0   5'-Guanylic Acid/*analogs & derivatives Prodrugs. Antimicrob Agents Chemother. 2011 Jan;55(1):76-81
retinoyl glutamate  0   *Glutamates *Tretinoin Prodrugs. J Pharm Pharmacol. 2009 Oct;61(10):1353-8
BP-PM279G  0   *Pyrrolidines Prodrugs. Org Lett. 2009 Aug 6;11(15):3394-7
BP-PM6  0   *Heterocyclic Compounds, 3-Ring Prodrugs. Org Lett. 2009 Aug 6;11(15):3394-7
chitosan-O-isopropyl-5'-O-d4T monophosphate conjugate  0   *Stavudine *Chitosan Prodrugs. Bioorg Med Chem Lett. 2009 May 1;19(9):2566-9
2-amino-N-(2-methyl-5-(1-(4-sulfamoylphenyl)-3-(trifluoromethyl)-1H-pyrazol-5-yl)phenyl)acetamide hydrochloride  0   *Pyrazoles Prodrugs. Biol Pharm Bull. 2009 Jun;32(6):1032-6
R1626  0   *Nucleosides Prodrugs. Drug Dev Ind Pharm. 2008 Jul;34(7):683-91
DG17 compound  0   Ritonavir/*analogs & derivatives Prodrugs. Curr HIV Res 2008 May;6(3):272-5
AWO54  0   Methotrexate/*analogs & derivatives Prodrugs. Ann Rheum Dis. 2008 Aug;67(8):1188-91
DTS-108  0   *Peptides Camptothecin/*analogs & derivatives Prodrugs. Clin Cancer Res 2008 Apr 1;14(7):2145-53
SN 28343  0   *Nitrogen Mustard Compounds Prodrugs. Cancer Gene Ther 2007 Dec;14(12):953-67
FV-100  0   *Pyrimidine Nucleosides Prodrugs. J Antimicrob Chemother 2007 Dec;60(6):1316-30
UNIL088  0   *Cyclosporins Prodrugs. Eur J Pharm Biopharm. 2007 Sep;67(2):555-61
R788 compound  0   *Oxazines *Pyridines Prodrugs. Clin Immunol 2007 Sep;124(3):244-57
2-(4-((5,6-diphenylpyrazin-2-yl)(isopropyl)amino)butoxy)-N-(methylsulfonyl)acetamide  0   *Acetamides *Pyrazines Prodrugs. J Pharmacol Exp Ther 2007 Sep;322(3):1181-8
temozolomide hexyl ester  0   Dacarbazine/*analogs & derivatives Prodrugs. J Pharm Pharmacol 2007 Jun;59(6):787-94
glycine-valine-saquinavir  0   Saquinavir/*analogs & derivatives Prodrugs. Int J Pharm 2007 May 24;336(2):233-40
valine-valine-saquinavir  0   Saquinavir/*analogs & derivatives Prodrugs. Int J Pharm 2007 May 24;336(2):233-40
A-322278  0   *Pyrrolidines Prodrugs. J Infect Dis 2006 Mar 15;193(6):765-72
LEG-3 prodrug  0   *Oligopeptides Doxorubicin/*analogs & derivatives Prodrugs. Cancer Res 2006 Jan 15;66(2):970-80
((O,O-diacetyl)-L-dopa-methylester)succinyldiamide  0   *Amides Levodopa/*analogs & derivatives Prodrugs. J Control Release. 2004 Sep 30;99(2):293-300
hydroxymethylnitrofurazone  0   Nitrofurazone/*analogs & derivatives Prodrugs. Bioorg Med Chem. 2003 Nov 3;11(22):4779-
AVE 7688  0   *Heterocyclic Compounds, 3-Ring Prodrugs. J Renin Angiotensin Aldosterone Syst. 2003 Sep;4(3):191-6
dabigatran etexilate  211915-06-9 3-((2-((4-amino((E)-hexyloxycarbonylimino)methyl)-phenylamino)methyl-1-1H-benzoimidazole-5-carbonyl)pyridin-2-yl-amino)propionic acid ethyl ester  *Benzimidazoles *Pyridines Prodrugs Antithrombin Proteins. J Med Chem 2002 Apr 25;45(9):1757-66PRADAXA
BIBR 953  0   *Benzimidazoles *Pyridines Prodrugs. J Med Chem 2002 Apr 25;45(9):1757-66
5-Fluoroindole-3-acetic acid  0   *Indoleacetic Acids Prodrugs. Biochem Pharmacol 2002 Jan 15;63(2):265-72
nalbuphine pivalate  0   Nalbuphine/*analogs & derivatives Prodrugs. Arzneimittelforschung 2001 51(5):408-13
dipivalyl terbutalone  0   *Pentanoic Acids Prodrugs Terbutaline. Drud Dev Ind Pharm 2001 Feb;27(2):137-41
L 377202  0   *Oligopeptides Doxorubicin/*analogs & derivatives Prodrugs. Nat Med 2000 Nov;6(11):1248-52
bispivaloylthioethyl zidovudine monophosphate  0   *Dideoxynucleotides Zidovudine/*analogs & derivatives Prodrugs. antiviral Chaem Chemother 2000 May;11(3):203-12
capecitabine  154361-50-9   Deoxycytidine/*analogs & derivatives Fluorouracil/*analogs & derivatives Prodrugs.
Pharma Action Antimetabolites, Antineoplastic
Cancer Res 1998 Feb 15;58(4):685-90XELODA
EM 800  0   *Benzopyrans *Propionates Prodrugs Stereoisomerism.
Pharma Action Estrogen Antagonists
J Med Chem 1997 Jul 4;40(14):2117-22
sibrafiban  0   *Oximes *Piperidines Prodrugs Platelet Glycoprotein GPIIb-IIIa Complex/antagonists & inhibitors.
Pharma Action Platelet Aggregation Inhibitors
J Med Chem 1996 Aug 2;39(16):3139-47
5-(1-aziridinyl)-2,4-dinitrobenzamide  21919-05-1   *Aziridines Prodrugs.
Pharma Action Antineoplastic Agents ; Radiation-Sensitizing Agents
tazarotene  118292-40-3 3-Pyridinecarboxylic acid, 6-((3,4-dihydro-4,4-dimethyl-2H-1-benzothiopyran-6-yl)ethynyl)-, ethyl ester  *Nicotinic Acids Gels Prodrugs Retinoids.
Pharma Action Dermatologic Agents ; Keratolytic Agents ; Teratogens
J Am Acad Dermatol 1994 Apr;30(4):581-90TAZORAC; AVAGE
valacyclovir  124832-27-5   Acyclovir/*analogs & derivatives Valine/*analogs & derivatives Prodrugs.
Pharma Action Antiviral Agents
J Med Virol 1993;Suppl 1:139-45VALACYCLOVIR HYDROCHLORIDE; VALTREX
S 1108  105889-45-0 5-Thia-1-azabicyclo(4.2.0)oct-2-ene-2-carboxylic acid, 3-(((aminocarbonyl)oxy)methyl)-7-((2-(2-amino-4-thiazolyl)-1-oxo-2-pentenyl)amino)-8-oxo-, (2,2-dimethyl-1-oxopropoxy)methyl ester, (6R-(6alpha,7beta(Z)))  *Cephalosporins Prodrugs. Antimicrob Agents Chemother 1992 Apr;36(4):757-61
RB 101  135949-60-9 L-Phenylalanine, N-(2-(((2-amino-4-(methylthio)butyl)dithio)methyl)-1-oxo-3-phenylpropyl)-, phenylmethyl ester  *Disulfides Phenylalanine/*analogs & derivatives Prodrugs.
Pharma Action Analgesics ; Enzyme Inhibitors
J Pharmacol Exp Ther 1992 Apr;261(1):181-90
RB 6145  122178-49-8   *Nitroimidazoles Prodrugs.
Pharma Action Radiation-Sensitizing Agents
J Med Chem 1991;34(3):1207
propacetamol  66532-86-3   Acetaminophen/*analogs & derivatives Prodrugs.
Pharma Action Analgesics ; Anti-Inflammatory Agents, Non-Steroidal
Cah Anesthesiol 1989;37(7):521
mycophenolate mofetil  128794-94-5   Mycophenolic Acid/*analogs & derivatives Anti-Inflammatory Agents, Non-Steroidal Antineoplastic Agents Dermatologic Agents Enzyme Inhibitors IMP Dehydrogenase/antagonists & inhibitors Prodrugs.
Pharma Action Immunosuppressive Agents
JAMA 1990;263(9):1184CELLCEPT; MYCOPHENOLATE MOFETIL; MYCOPHENOLATE MOFETIL HYDROCHLORIDE
candoxatril  118785-03-8   *Indans *Propionates Prodrugs Neprilysin/antagonists & inhibitors.
Pharma Action Antihypertensive Agents ; Protease Inhibitors
Br J Pharmacol 1989;98 Suppl:823P
famciclovir  104227-87-4   2-Aminopurine/*analogs & derivatives Prodrugs.
Pharma Action Antiviral Agents
J Med Chem 1989;32(8):1738FAMVIR; FAMCICLOVIR
erythromycin 2'-acetate  992-69-8   Erythromycin/*analogs & derivatives Prodrugs. J Antimicrob Chemother 1988;21 Suppl D:9
cefpodoxime proxetil  87239-81-4   Ceftizoxime/*analogs & derivatives Prodrugs.
Pharma Action Anti-Bacterial Agents
Antimicrob Agents Chemother 1987;31(7):1085VANTIN; CEFPODOXIME PROXETIL; BANAN
do carpamine  74639-40-0   Dopamine/*analogs & derivatives Prodrugs.
Pharma Action Dopamine Agonists
Masui 1986;35(12):1824
irinotecan  100286-90-6   Camptothecin/*analogs & derivatives Prodrugs.
Pharma Action Antineoplastic Agents, Phytogenic ; Radiation-Sensitizing Agents ; Topoisomerase I Inhibitors
Gan To Kagaku Ryoho 1987;14(3 Pt 2):850IRINOTECAN HYDROCHLORIDE; CAMPTOSAR
bambuterol  81732-65-2   Terbutaline/*analogs & derivatives Delayed-Action Preparations Prodrugs.
Pharma Action Bronchodilator Agents
Eur J Clin Pharmacol 1985;29(4):425
fosinoprilic acid  95399-71-6 L-Proline, 4-cyclohexyl-1-((hydroxy(4-phenylbutyl)phosphinyl)acetyl)-, trans  Fosinopril/*analogs & derivatives Prodrugs.
Pharma Action Angiotensin-Converting Enzyme Inhibitors ; Anti-Arrhythmia Agents ; Antihypertensive Agents
Anal Biochem 1985;148(2):401
fosphenytoin  93390-81-9 2,4-Imidazolidinedione, 5,5-diphenyl-3-((phosphonooxy)methyl)-, (SP-4-2)  Phenytoin/*analogs & derivatives Prodrugs.
Pharma Action Anticonvulsants
J Pharm Sci 1984;73(8):1080; J Pharm Sci 1984;73(8):1087CEREBYX; FOSPHENYTOIN SODIUM
desciclovir  84408-37-7 Ethanol, 2-((2-amino-9H-purin-9-yl)methoxy)  Acyclovir/*analogs & derivatives Prodrugs.
Pharma Action Antiviral Agents
Natl Proc Acad Sci USA 1984;81(10):3209
balsalazide  82101-18-6 Benzoic acid, 5-((4-(((2-carboxyethyl)amino)carbonyl)phenyl)azo)-2-hydroxy-, disodium salt  *Phenylhydrazines *Mesalamine Colitis, Ulcerative Prodrugs Inflammatory Bowel Diseases.
Pharma Action Anti-Inflammatory Agents, Non-Steroidal ; Gastrointestinal Agents
Dig Dis Sci 1983;28(7):609COLAZAL; GIAZO; BALSALAZIDE DISODIUM
fluphenazine depot  5002-47-1   Fluphenazine/*analogs & derivatives Delayed-Action Preparations Prodrugs.
Pharma Action Antipsychotic Agents
Ann Med Psychol (Paris) 2(4):642;1976; C R Soc Biol (Paris) 1979;173(4):979; Cur Ther Res 20(2):177;1976; Farmakol Toksikol 38(4):393;1975; Pol Tyg Lek 32(44):1725;1977; Psychiatr Pol 10(5):479;1976; Vrach Delo 1980;(1):93FLUPHENAZINE; PROLIXIN DECANOATE; FLUPHENAZINE DECANOATE
prednisolone acetate  52-21-1   Prednisolone/*analogs & derivatives Prodrugs.
Pharma Action Anti-Inflammatory Agents
Z Urol Nephrol 67(8):613;1974PRED FORTE; OMNIPRED; METICORTELONE; STERANE; ECONOPRED; PRED MILD; FLO-PRED; PREDNISOLONE ACETATE
5-fluoropyrimidin-2-one  2022-78-8   *Pyrimidinones Prodrugs. Biochem Pharmacol 21(18):2451;1972

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Sources: NLM Medical Subject Headings, NIH UMLS, Drugs@FDA, FDA AERS original data copyright United States Government. No endorsement implied. Last modified 6/6/2012

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