ZIDOVUDINE

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C10H13N5O4
Molecular Weight	267.2413
Optical Activity	UNSPECIFIED
Defined Stereocenters	3 / 3
E/Z Centers	1
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CC1=CN([C@H]2C[C@H](N=[N+]=[N-])[C@@H](CO)O2)C(=O)NC1=O

InChI

InChIKey=HBOMLICNUCNMMY-XLPZGREQSA-N

InChI=1S/C10H13N5O4/c1-5-3-15(10(18)12-9(5)17)8-2-6(13-14-11)7(4-16)19-8/h3,6-8,16H,2,4H2,1H3,(H,12,17,18)/t6-,7+,8+/m0/s1

HIDE SMILES / InChI

Molecular Formula	C10H13N5O4
Molecular Weight	267.2413
Charge	0
Count

Stereochemistry	ABSOLUTE
Additional Stereochemistry	No
Defined Stereocenters	3 / 3
E/Z Centers	1
Optical Activity	UNSPECIFIED

Description
Sources: https://www.drugbank.ca/drugs/DB00495
Curator's Comment: Description was created based on several sources, including https://www.accessdata.fda.gov/drugsatfda_docs/label/2008/019910s033lbl.pdf

Zidovudine is a nucleoside reverse transcriptase inhibitor (NRTI) with activity against Human Immunodeficiency Virus Type 1 (HIV-1). Zidovudine is phosphorylated to active metabolites that compete for incorporation into viral DNA. They inhibit the HIV reverse transcriptase enzyme competitively and act as a chain terminator of DNA synthesis. The lack of a 3'-OH group in the incorporated nucleoside analogue prevents the formation of the 5' to 3' phosphodiester linkage essential for DNA chain elongation, and therefore, the viral DNA growth is terminated. Zidovudine, a structural analog of thymidine, is a prodrug that must be phosphorylated to its active 5′-triphosphate metabolite, zidovudine triphosphate (ZDV-TP). It inhibits the activity of HIV-1 reverse transcriptase (RT) via DNA chain termination after incorporation of the nucleotide analogue. It competes with the natural substrate dGTP and incorporates itself into viral DNA. It is also a weak inhibitor of cellular DNA polymerase α and γ. Zidovudine is used in combination with other antiretroviral agents for the treatment of human immunovirus (HIV) infections. Zidovudine is marketed as Retrovir.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Potency
DU-145 2 Target ID: CHEMBL613508 Sources: https://www.ncbi.nlm.nih.gov/pubmed/12893431	Inhibitor 8504	24.0 µM [IC50]
MCF7 22 Target ID: CHEMBL387 Sources: https://www.ncbi.nlm.nih.gov/pubmed/12893431	Inhibitor 8504	22.0 µM [IC50]
Human immunodeficiency virus type 1 reverse transcriptase 70 Target ID: CHEMBL247 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2008/019910s033lbl.pdf \| https://www.ncbi.nlm.nih.gov/pubmed/24794751 \| https://www.ncbi.nlm.nih.gov/pubmed/9001825	Inhibitor 8504	0.01 µM [EC50]

Conditions

Condition	Modality	Targets	Highest Phase	Product
HIV-1 infection 156 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2008/019910s033lbl.pdf	Primary		Approved 8583	RETROVIR Approved Use RETROVIR is a nucleoside analogue reverse transcriptase inhibitor indicated for: -- Treatment of Human Immunodeficiency Virus (HIV-1) infection in combination with other antiretroviral agents. (1.1) -- Prevention of maternal-fetal HIV-1 transmission. (1.2) Launch Date 1987

C_max

Value	Dose	Analyte	Population
0.16 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1803995	50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered:	ZIDOVUDINE serum	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
0.2 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1803995	50 mg 6 times / day steady-state, oral dose: 50 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	ZIDOVUDINE serum	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
0.74 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1803995	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	ZIDOVUDINE serum	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
0.55 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1803995	100 mg 6 times / day steady-state, oral dose: 100 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	ZIDOVUDINE serum	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
1.72 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1803995	150 mg single, intravenous dose: 150 mg route of administration: Intravenous experiment type: SINGLE co-administered:	ZIDOVUDINE serum	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
1 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1803995	250 mg single, oral dose: 250 mg route of administration: Oral experiment type: SINGLE co-administered:	ZIDOVUDINE serum	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
1 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1803995	250 mg 6 times / day steady-state, oral dose: 250 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	ZIDOVUDINE serum	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
1.8 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1803995	150 mg 6 times / day steady-state, intravenous dose: 150 mg route of administration: Intravenous experiment type: STEADY-STATE co-administered:	ZIDOVUDINE serum	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
1.1 μg/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/019910s041lbl.pdf	2.5 mg/kg 6 times / day steady-state, intravenous dose: 2.5 mg/kg route of administration: Intravenous experiment type: STEADY-STATE co-administered:	ZIDOVUDINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN

AUC

Value	Dose	Analyte	Population
0.26 mg × h/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1803995	50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered:	ZIDOVUDINE serum	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
0.32 mg × h/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1803995	50 mg 6 times / day steady-state, oral dose: 50 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	ZIDOVUDINE serum	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
0.39 mg × h/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1803995	60 mg single, intravenous dose: 60 mg route of administration: Intravenous experiment type: SINGLE co-administered:	ZIDOVUDINE serum	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
0.74 mg × h/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1803995	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	ZIDOVUDINE serum	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
0.65 mg × h/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1803995	100 mg 6 times / day steady-state, oral dose: 100 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	ZIDOVUDINE serum	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
1.22 mg × h/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1803995	150 mg single, intravenous dose: 150 mg route of administration: Intravenous experiment type: SINGLE co-administered:	ZIDOVUDINE serum	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
1.33 mg × h/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1803995	250 mg single, oral dose: 250 mg route of administration: Oral experiment type: SINGLE co-administered:	ZIDOVUDINE serum	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
1.28 mg × h/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1803995	250 mg 6 times / day steady-state, oral dose: 250 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	ZIDOVUDINE serum	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
1.31 mg × h/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1803995	150 mg 6 times / day steady-state, intravenous dose: 150 mg route of administration: Intravenous experiment type: STEADY-STATE co-administered:	ZIDOVUDINE serum	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
1400 ng × h/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/019910s041lbl.pdf	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:	ZIDOVUDINE plasma	Homo sapiens population: UNKNOWN age: ADULT sex: UNKNOWN food status: UNKNOWN

T_1/2

Value	Dose	Analyte	Population
1.5 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1803995	50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered:	ZIDOVUDINE serum	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
1.4 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1803995	50 mg 6 times / day steady-state, oral dose: 50 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	ZIDOVUDINE serum	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
1.3 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1803995	60 mg single, intravenous dose: 60 mg route of administration: Intravenous experiment type: SINGLE co-administered:	ZIDOVUDINE serum	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
1.6 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1803995	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	ZIDOVUDINE serum	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
1.1 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1803995	100 mg 6 times / day steady-state, oral dose: 100 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	ZIDOVUDINE serum	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
1.7 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1803995	150 mg single, intravenous dose: 150 mg route of administration: Intravenous experiment type: SINGLE co-administered:	ZIDOVUDINE serum	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
1.5 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1803995	250 mg single, oral dose: 250 mg route of administration: Oral experiment type: SINGLE co-administered:	ZIDOVUDINE serum	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
1.1 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1803995	250 mg 6 times / day steady-state, oral dose: 250 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	ZIDOVUDINE serum	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
1.4 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1803995	150 mg 6 times / day steady-state, intravenous dose: 150 mg route of administration: Intravenous experiment type: STEADY-STATE co-administered:	ZIDOVUDINE serum	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
1 h DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/019910s041lbl.pdf	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:	ZIDOVUDINE plasma	Homo sapiens population: UNKNOWN age: ADULT sex: UNKNOWN food status: UNKNOWN

F_unbound

Value	Dose	Co-administered	Analyte	Population
62% DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/019910s041lbl.pdf	2.5 mg/kg 6 times / day steady-state, intravenous dose: 2.5 mg/kg route of administration: Intravenous experiment type: STEADY-STATE co-administered:		ZIDOVUDINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN

Doses

Dose	Population	Adverse events
20000 mg single, oral Overdose Dose: 20000 mg Route: oral Route: single Dose: 20000 mg Sources: https://pubmed.ncbi.nlm.nih.gov/3163102/	unhealthy, 28 years Health Status: unhealthy Age Group: 28 years Sex: M Sources: https://pubmed.ncbi.nlm.nih.gov/3163102/	Disc. AE: Anemia... AEs leading to discontinuation/dose reduction: Anemia (grade 1, 1 patient) Sources: https://pubmed.ncbi.nlm.nih.gov/3163102/
1000 mg 1 times / day steady, oral Highest studied dose Dose: 1000 mg, 1 times / day Route: oral Route: steady Dose: 1000 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/2036464/	unhealthy, 34 years Health Status: unhealthy Age Group: 34 years Sex: M Sources: https://pubmed.ncbi.nlm.nih.gov/2036464/	Other AEs: Depression... Other AEs: Depression (1 patient) Sources: https://pubmed.ncbi.nlm.nih.gov/2036464/
22.5 g single, oral Overdose Dose: 22.5 g Route: oral Route: single Dose: 22.5 g Sources: https://pubmed.ncbi.nlm.nih.gov/2036464/	unhealthy, 34 years Health Status: unhealthy Age Group: 34 years Sex: M Sources: https://pubmed.ncbi.nlm.nih.gov/2036464/	Disc. AE: Dizziness, Diarrhoea... AEs leading to discontinuation/dose reduction: Dizziness (1 patient) Diarrhoea (1 patient) Sources: https://pubmed.ncbi.nlm.nih.gov/2036464/
20000 mg single, oral Overdose Dose: 20000 mg Route: oral Route: single Dose: 20000 mg Sources: https://pubmed.ncbi.nlm.nih.gov/2900428/	unhealthy, 34 years Health Status: unhealthy Age Group: 34 years Sex: M Sources: https://pubmed.ncbi.nlm.nih.gov/2900428/	Disc. AE: Drowsiness... AEs leading to discontinuation/dose reduction: Drowsiness (1 patient) Sources: https://pubmed.ncbi.nlm.nih.gov/2900428/
36 g single, oral Overdose Dose: 36 g Route: oral Route: single Dose: 36 g Sources: https://pubmed.ncbi.nlm.nih.gov/2563536/	unhealthy, 35 years Health Status: unhealthy Age Group: 35 years Sex: M Sources: https://pubmed.ncbi.nlm.nih.gov/2563536/	Disc. AE: Seizure... AEs leading to discontinuation/dose reduction: Seizure (1 patient) Sources: https://pubmed.ncbi.nlm.nih.gov/2563536/
134 mg single, oral Overdose Dose: 134 mg Route: oral Route: single Dose: 134 mg Sources: https://pubmed.ncbi.nlm.nih.gov/21867364/	healthy, 4 day Health Status: healthy Age Group: 4 day Sex: F Sources: https://pubmed.ncbi.nlm.nih.gov/21867364/	Disc. AE: Metabolic acidosis exacerbated... AEs leading to discontinuation/dose reduction: Metabolic acidosis exacerbated (1 patient) Sources: https://pubmed.ncbi.nlm.nih.gov/21867364/
8000 mg/m2 multiple, intravenous MTD Dose: 8000 mg/m2 Route: intravenous Route: multiple Dose: 8000 mg/m2 Sources: https://pubmed.ncbi.nlm.nih.gov/9261522/	unhealthy, adult Health Status: unhealthy Age Group: adult Sex: unknown Sources: https://pubmed.ncbi.nlm.nih.gov/9261522/	Disc. AE: Cardiac arrhythmia... Other AEs: Diarrhea... AEs leading to discontinuation/dose reduction: Cardiac arrhythmia (grade 5, 1 patient) Other AEs: Diarrhea (grade 3-4, 17%) Sources: https://pubmed.ncbi.nlm.nih.gov/9261522/
40 g single, oral Overdose Dose: 40 g Route: oral Route: single Dose: 40 g Sources: https://pubmed.ncbi.nlm.nih.gov/2563536/	unhealthy, adult Health Status: unhealthy Age Group: adult Sex: unknown Sources: https://pubmed.ncbi.nlm.nih.gov/2563536/	Disc. AE: Nystagmus... AEs leading to discontinuation/dose reduction: Nystagmus (1 patient) Sources: https://pubmed.ncbi.nlm.nih.gov/2563536/
500 mg 1 times / day steady, oral Recommended Dose: 500 mg, 1 times / day Route: oral Route: steady Dose: 500 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2008/019910s033lbl.pdf	unhealthy, adult Health Status: unhealthy Age Group: adult Sex: unknown Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2008/019910s033lbl.pdf	Other AEs: Asthenia, Headache... Other AEs: Asthenia (9%) Headache (63%) Malaise (53%) Anorexia (20%) Constipation (6%) Nausea (51%) Vomiting (17%) Anemia (1%) Granulocytopenia (2%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2008/019910s033lbl.pdf
160 mg/m2 3 times / day steady, oral Recommended Dose: 160 mg/m2, 3 times / day Route: oral Route: steady Dose: 160 mg/m2, 3 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2008/019910s033lbl.pdf	unhealthy, children Health Status: unhealthy Age Group: children Sex: unknown Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2008/019910s033lbl.pdf	Other AEs: Fever, Hepatomegaly... Other AEs: Fever (25%) Hepatomegaly (11%) Nausea and vomiting (8%) Diarrhea (8%) Stomatitis (6%) Splenomegaly (5%) Cough (15%) Breath sounds abnormal (7%) Ear disorders NEC (7%) Congestion nasal (8%) Skin rash (12%) Lymphadenopathy (9%) Neutropenia (8%) Thrombocytopenia (1%) ALT (grade 3, 1%) Lipase (3%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2008/019910s033lbl.pdf

AEs

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
substrate 1946 inhibitor 2252	substrate 1193 inhibitor 2438	inhibitor 2507	inhibitor 2217

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
UGT 45 P-gp 1741 BCRP 910 OAT3 747 MRP2 499 MRP3 246 MRP4 290 CYP1A2 2153 CYP2A6 879 CYP2C19 2057 CYP2E1 1060 OAT1 725 OAT2 153 OAT4 150 OCT1 620 OCT2 779 OCTN2 71 OATP1B1 1079 OATP1B3 961 OATP2B1 157 MRP1 116	UGT 219 UGT1A1 479 UGT1A3 470 UGT1A4 399 UGT1A6 343 UGT1A7 249 UGT1A9 423 UGT1A10 331 UGT2B4 278 UGT2B7 456 UGT2B15 236 UGT2B17 237 CYP2A6 626 CYP2C8 810 CYP2C19 1119 P-gp 2052 MRP4 91 MRP5 41 BCRP 697 OAT1 395 OAT2 125 OAT3 391 OAT4 93 OCT2 434

Drug as perpetrator

Target	Modality	Activity
BCRP 985	inhibitor 4027 Sources: https://pubmed.ncbi.nlm.nih.gov/28712845/, https://pubmed.ncbi.nlm.nih.gov/23956101/	no [IC50 <400 uM]
P-gp 1932	inhibitor 4027 Sources: https://pubmed.ncbi.nlm.nih.gov/28712845/	no [IC50 <500 uM]
CYP1A2 2333	inhibitor 4027 Sources: https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkwzMzU2IiwidXNlX2N1c3RvbV9xdWVyeSI6dHJ1ZSwic2VhcmNoX3Rlcm0iOiIiLCJ0ZXh0X2ZpbHRlciI6IkNIRU1CTDEyOSJ9fQ%3D%3D	no [IC50 >10 uM]
CYP2A6 911	inhibitor 4027 Sources: https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkw1MjgyIiwidXNlX2N1c3RvbV9xdWVyeSI6dHJ1ZSwic2VhcmNoX3Rlcm0iOiIiLCJ0ZXh0X2ZpbHRlciI6IkNIRU1CTDEyOSJ9fQ%3D%3D	no [IC50 >10 uM]
CYP2C19 2141	inhibitor 4027 Sources: https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkwzNjIyIiwidXNlX2N1c3RvbV9xdWVyeSI6dHJ1ZSwic2VhcmNoX3Rlcm0iOiIiLCJ0ZXh0X2ZpbHRlciI6IkNIRU1CTDEyOSJ9fQ%3D%3D	no [IC50 >10 uM]
CYP2C9 2497	inhibitor 4027 Sources: https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkwzMzk3IiwidXNlX2N1c3RvbV9xdWVyeSI6dHJ1ZSwic2VhcmNoX3Rlcm0iOiIiLCJ0ZXh0X2ZpbHRlciI6IkNIRU1CTDEyOSJ9fQ%3D%3D	no [IC50 >10 uM]
CYP2D6 2546	inhibitor 4027 Sources: https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkwyODkiLCJ1c2VfY3VzdG9tX3F1ZXJ5Ijp0cnVlLCJzZWFyY2hfdGVybSI6IiIsInRleHRfZmlsdGVyIjoiQ0hFTUJMMTI5In19	no [IC50 >10 uM]
CYP2E1 1146	inhibitor 4027 Sources: https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkw1MjgxIiwidXNlX2N1c3RvbV9xdWVyeSI6dHJ1ZSwic2VhcmNoX3Rlcm0iOiIiLCJ0ZXh0X2ZpbHRlciI6IkNIRU1CTDEyOSJ9fQ%3D%3D	no [IC50 >10 uM]
CYP3A4 2633	inhibitor 4027 Sources: https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkwzNDAiLCJ1c2VfY3VzdG9tX3F1ZXJ5Ijp0cnVlLCJzZWFyY2hfdGVybSI6IiIsInRleHRfZmlsdGVyIjoiQ0hFTUJMMTI5In19	no [IC50 >10 uM]
MRP2 625	inhibitor 4027 Sources: https://pubmed.ncbi.nlm.nih.gov/23956101/	no [IC50 >133 uM]
MRP3 326	inhibitor 4027 Sources: https://pubmed.ncbi.nlm.nih.gov/23956101/	no [IC50 >133 uM]
MRP4 345	inhibitor 4027 Sources: https://pubmed.ncbi.nlm.nih.gov/23956101/	no [IC50 >133 uM]
MRP1 232	inhibitor 4027 Sources: https://journals.lww.com/aidsonline/Fulltext/2002/09060/The_protease_inhibitor_ritonavir_inhibits_the.5.aspx, https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkwzMDA0IiwidXNlX2N1c3RvbV9xdWVyeSI6dHJ1ZSwic2VhcmNoX3Rlcm0iOiIiLCJ0ZXh0X2ZpbHRlciI6IkNIRU1CTDEyOSJ9fQ%3D%3D	no
OATP2B1 162	inhibitor 4027 Sources: https://pubs.acs.org/doi/10.1021/jm300212s	no
OCT1 656	inhibitor 4027 Sources: https://pubmed.ncbi.nlm.nih.gov/11861798/	no
OCT2 782	inhibitor 4027 Sources: https://pubmed.ncbi.nlm.nih.gov/11861798/	no
OCTN2 71	inhibitor 4027 Sources: https://pubmed.ncbi.nlm.nih.gov/10525100/, https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkwyMDczNjkzIiwidXNlX2N1c3RvbV9xdWVyeSI6dHJ1ZSwic2VhcmNoX3Rlcm0iOiIiLCJ0ZXh0X2ZpbHRlciI6IkNIRU1CTDEyOSJ9fQ%3D%3D	no
OAT3 749	inhibitor 4027 Sources: https://pubmed.ncbi.nlm.nih.gov/30928510/, https://pubmed.ncbi.nlm.nih.gov/11861798/, https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkwxNjQxMzQ4IiwidXNlX2N1c3RvbV9xdWVyeSI6dHJ1ZSwic2VhcmNoX3Rlcm0iOiIiLCJ0ZXh0X2ZpbHRlciI6IkNIRU1CTDEyOSJ9fQ%3D%3D	weak [IC50 31.34 uM]
UGT 70	inhibitor 4027 Sources: https://pubmed.ncbi.nlm.nih.gov/1907149/	yes [Ki 1200 uM]
OAT1 730	inhibitor 4027 Sources: https://pubmed.ncbi.nlm.nih.gov/11861798/, https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkwxNjQxMzQ3IiwidXNlX2N1c3RvbV9xdWVyeSI6dHJ1ZSwic2VhcmNoX3Rlcm0iOiIiLCJ0ZXh0X2ZpbHRlciI6IkNIRU1CTDEyOSJ9fQ%3D%3D	yes
OAT2 155	inhibitor 4027 Sources: https://pubmed.ncbi.nlm.nih.gov/11861798/, https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkwxOTU1NzExIiwidXNlX2N1c3RvbV9xdWVyeSI6dHJ1ZSwic2VhcmNoX3Rlcm0iOiIiLCJ0ZXh0X2ZpbHRlciI6IkNIRU1CTDEyOSJ9fQ%3D%3D	yes
OAT4 150	inhibitor 4027 Sources: https://pubmed.ncbi.nlm.nih.gov/11861798/, https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkwyMDczNjc3IiwidXNlX2N1c3RvbV9xdWVyeSI6dHJ1ZSwic2VhcmNoX3Rlcm0iOiIiLCJ0ZXh0X2ZpbHRlciI6IkNIRU1CTDEyOSJ9fQ%3D%3D	yes
OATP1B1 1095	inhibitor 4027 Sources: https://pubmed.ncbi.nlm.nih.gov/23571415/	yes
OATP1B3 970	inhibitor 4027 Sources: https://pubmed.ncbi.nlm.nih.gov/23571415/	yes

Drug as victim

Target	Modality	Activity	Clinical evidence
UGT2B7 456	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/12920168/, https://pubmed.ncbi.nlm.nih.gov/19628728/	major [Km 770 uM]	yes (pharmacogenomic study) Comment: Km (Pooled HLMs) = 1.4 mM; The carriers of UGT2B7*1c had 57% lower mean AUC (P = 0.029, unpaired t-test), 196% higher mean CL/F (P = 0.004, unpaired t-test) (Figure 3B), and 67% shorter mean elimination half-life (P = 0.030, unpaired t-test) compared with non-carriers. Sources: https://pubmed.ncbi.nlm.nih.gov/12920168/, https://pubmed.ncbi.nlm.nih.gov/19628728/
UGT2B15 236	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/12920168/	minor
UGT2B4 278	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/12920168/	minor
OCT2 434	substrate 4014 Sources: https://jasn.asnjournals.org/content/13/7/1703, https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkwxNzQzMTIyIiwidXNlX2N1c3RvbV9xdWVyeSI6dHJ1ZSwic2VhcmNoX3Rlcm0iOiIiLCJ0ZXh0X2ZpbHRlciI6IkNIRU1CTDEyOSJ9fQ%3D%3D	no
UGT1A1 479	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/12920168/	no
UGT1A10 331	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/12920168/	no
UGT1A3 470	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/12920168/	no
UGT1A4 399	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/12920168/	no
UGT1A6 343	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/12920168/	no
UGT1A7 249	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/12920168/	no
UGT1A9 423	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/12920168/	no
UGT2B17 237	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/12920168/	no
OAT3 391	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/11861798/, https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkwxNjQxMzQ4IiwidXNlX2N1c3RvbV9xdWVyeSI6dHJ1ZSwic2VhcmNoX3Rlcm0iOiIiLCJ0ZXh0X2ZpbHRlciI6IkNIRU1CTDEyOSJ9fQ%3D%3D	yes [Km 145.1 uM]
OAT4 93	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/11861798/, https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkwyMDczNjc3IiwidXNlX2N1c3RvbV9xdWVyeSI6dHJ1ZSwic2VhcmNoX3Rlcm0iOiIiLCJ0ZXh0X2ZpbHRlciI6IkNIRU1CTDEyOSJ9fQ%3D%3D	yes [Km 151.8 uM]
UGT 219	substrate 4014 Sources: https://www.info.pmda.go.jp/go/interview/2/166272_6250001M1038_2_RVC_1F.pdf#page=23, https://pubmed.ncbi.nlm.nih.gov/1907149/, https://bioinformatics.charite.de/transformer/index.php?site=fullinfo&cname=030516871 Page: (PMDA drug information) 23	yes [Km 2400 uM]
OAT2 125	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/11861798/, https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkwxOTU1NzExIiwidXNlX2N1c3RvbV9xdWVyeSI6dHJ1ZSwic2VhcmNoX3Rlcm0iOiIiLCJ0ZXh0X2ZpbHRlciI6IkNIRU1CTDEyOSJ9fQ%3D%3D	yes [Km 26.8 uM]
OAT1 395	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/11861798/, https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkwxNjQxMzQ3IiwidXNlX2N1c3RvbV9xdWVyeSI6dHJ1ZSwic2VhcmNoX3Rlcm0iOiIiLCJ0ZXh0X2ZpbHRlciI6IkNIRU1CTDEyOSJ9fQ%3D%3D	yes [Km 45.9 uM]
BCRP 697	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/18464048/, https://pubmed.ncbi.nlm.nih.gov/15345326/	yes
CYP2A6 626	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/11996015/	yes
CYP2C19 1119	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/11996015/	yes
CYP2C8 810	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/11996015/	yes
CYP2C9 1193	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/11996015/	yes
CYP3A4 1946	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/11996015/	yes
MRP4 91	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/18535159/	yes
MRP5 41	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/18535159/	yes
P-gp 2052	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/19472342/	yes

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
hERG 2263	inhibitor 2237 Sources: https://www.ebi.ac.uk/chembl/g/#browse/activities/full_state/eyJsaXN0Ijp7InNldHRpbmdzX3BhdGgiOiJFU19JTkRFWEVTX05PX01BSU5fU0VBUkNILkFDVElWSVRZIiwiY3VzdG9tX3F1ZXJ5IjoidGFyZ2V0X2NoZW1ibF9pZDpDSEVNQkwyNDAiLCJ1c2VfY3VzdG9tX3F1ZXJ5Ijp0cnVlLCJzZWFyY2hfdGVybSI6IiIsInRleHRfZmlsdGVyIjoiQ0hFTUJMMTI5In19

Sourcing

Vendor/Aggregator	ID	URL
ChEBI	CHEBI:10110	https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:10110
eMolecules	479032	https://www.emolecules.com/cgi-bin/more?vid=479032
eMolecules	747869	https://www.emolecules.com/cgi-bin/more?vid=747869
MolPort	MolPort-002-507-286	https://www.molport.com/shop/molecule-link/MolPort-002-507-286
Selleck Chemicals	zidovudine-retrovir	http://www.selleckchem.com/products/zidovudine-retrovir.html
ZINC	ZINC000003779042	http://zinc15.docking.org/substances/ZINC000003779042

PubMed

Title	Date	PubMed
Anti-HIV activity and mechanism of action of macrocyclic diamide SRR-SB3.	1998 Dec	10052846
Antisense activity of an anti-HIV oligonucleotide conjugated to linear and branched high molecular weight polyethylene glycols.	1998 Oct-Nov	10205850
In vitro anti-hepatitis B virus activities of 5"-O-myristoyl analogue derivatives of 3"-fluoro-2",3"-dideoxythymidine (FLT) and 3"-azido-2",3"-dideoxythymidine (AZT).	1998 Sep-Dec	10948398
Synthesis of 4'-substituted nucleosides and their biological evaluation.	1999	10780412
Synthesis and anti-HIV activity of unusual nucleoside oxanosine derivatives.	1999	10780358
Zidovudine-associated type B lactic acidosis and hepatic steatosis in an HIV-infected patient.	1999 Apr	10219365
Chicoric acid analogues as HIV-1 integrase inhibitors.	1999 Apr 22	10212126
Synthesis and anti-HIV activity of some S-acyl-2-thioethyl (SATE) phosphoramidate derivatives of 3'-azido-2',3'-dideoxythymidine.	1999 Apr-May	10432724
A new point mutation (P157S) in the reverse transcriptase of human immunodeficiency virus type 1 confers low-level resistance to (-)-beta-2',3'-dideoxy-3'-thiacytidine.	1999 Aug	10428942
Unique anti-human immunodeficiency virus activities of the nonnucleoside reverse transcriptase inhibitors calanolide A, costatolide, and dihydrocostatolide.	1999 Aug	10428899
Synthesis and anti-HIV activity of 1,1,3-trioxo-2H,4H-thieno[3,4-e][1,2,4]thiadiazines (TTDs): a new family of HIV-1 specific non-nucleoside reverse transcriptase inhibitors.	1999 Dec	10658585
Charge modification of plasma and milk proteins results in antiviral active compounds.	1999 Dec	10628656
Substituted 7H-pyrido[4,3-c]carbazoles with potent anti-HIV activity.	1999 Jan 18	10021911
Relation of peripheral neuropathy to HIV treatment in four randomized clinical trials including didanosine.	1999 Jul	10463516
Biological evaluation of proanthocyanidin dimers and related polyphenols.	1999 Jul	10425115
A screening assay for antiviral compounds targeted to the HIV-1 gp41 core structure using a conformation-specific monoclonal antibody.	1999 Jun	10403680
Utilization of transgenic mice replicating high levels of hepatitis B virus for antiviral evaluation of lamivudine.	1999 Jun	10389653
In vitro anti-human immunodeficiency virus activities of Z- and E-methylenecyclopropane nucleoside analogues and their phosphoro-L-alaninate diesters.	1999 Jun	10348777
Rational design of N-[2-(2,5-dimethoxyphenylethyl)]-N'-[2-(5-bromopyridyl)]-thiourea (HI-236) as a potent non-nucleoside inhibitor of drug-resistant human immunodeficiency virus.	1999 Jun 7	10386942
Synthesis and biological evaluation of 2',3'-didehydro-2',3'- dideoxy-5-fluorocytidine (D4FC) analogues: discovery of carbocyclic nucleoside triphosphates with potent inhibitory activity against HIV-1 reverse transcriptase.	1999 Mar 11	10072683
A new class of anti-HIV agents: synthesis and activity of conjugates of HIV protease inhibitors with a reverse transcriptase inhibitor.	1999 Mar 22	10206539
Prolactin exerts hematopoietic growth-promoting effects in vivo and partially counteracts myelosuppression by azidothymidine.	1999 May	10340396
Multiorgan transplacental and neonatal carcinogenicity of 3'-azido-3'-deoxythymidine in mice.	1999 Nov 15	10558926
Synthesis of 2',3'-dideoxy-2'-fluoro-L-threo-pentofuranosyl nucleosides as potential antiviral agents.	1999 Oct	10616728
A novel genotype encoding a single amino acid insertion and five other substitutions between residues 64 and 74 of the HIV-1 reverse transcriptase confers high-level cross-resistance to nucleoside reverse transcriptase inhibitors. Abacavir CNA2007 International Study Group.	1999 Oct 1	10843527
The anti-HIV pseudopeptide HB-19 forms a complex with the cell-surface-expressed nucleolin independent of heparan sulfate proteoglycans.	1999 Sep 24	10488134
Long-term exposure of HIV type 1-infected cell cultures to combinations of the novel quinoxaline GW420867X with lamivudine, abacavir, and a variety of nonnucleoside reverse transcriptase inhibitors.	2000 Apr 10	10777142
Prevalence and characteristics of multinucleoside-resistant human immunodeficiency virus type 1 among European patients receiving combinations of nucleoside analogues.	2000 Aug	10898683
Importance of the alanine methyl ester side chain for the biological activity profile of dual-function phenyl phosphate derivatives of bromo-methoxy-zidovudine.	2000 Jan	10693652
Activities of masked 2',3'-dideoxynucleoside monophosphate derivatives against human immunodeficiency virus in resting macrophages.	2000 Jan	10602742
Antioxidant function of phenethyl-5-bromo-pyridyl thiourea compounds with potent anti-HIV activity.	2000 Jan 3	10636251
Synthesis and antiviral activity of amino acid carbamate derivatives of AZT.	2000 Jan-Feb	10772704
Cytochrome c oxidase deficiency in the muscle of patients with zidovudine myopathy is segmental and affects both mitochondrial DNA- and nuclear DNA-encoded subunits.	2000 Jul	10912924
In vitro selection of mutations in the human immunodeficiency virus type 1 reverse transcriptase that decrease susceptibility to (-)-beta-D-dioxolane-guanosine and suppress resistance to 3'-azido-3'-deoxythymidine.	2000 Jul	10858331
3-year suppression of HIV viremia with indinavir, zidovudine, and lamivudine.	2000 Jul 4	10877738
Presence of 2',5'-Bis-O-(tert-butyldimethylsilyl)-3'-spiro-5"-(4"-amino-1",2"-oxath iole-2",2"-dioxide) (TSAO)-resistant virus strains in TSAO-inexperienced HIV patients.	2000 Jun 10	10875608
'Double-Drugs'--a new class of prodrug form of an HIV protease inhibitor conjugated with a reverse transcriptase inhibitor by a spontaneously cleavable linker.	2000 Jun 5	10866387
Structure-activity relationship studies on potential non-nucleoside DABO-like inhibitors of HIV-1 reverse transcriptase.	2000 Mar	10819436
Coumarins and bicoumarin from Ferula sumbul: anti-HIV activity and inhibition of cytokine release.	2000 Mar	10746882
Spiropentane mimics of nucleosides: analogues of 2'-deoxyadenosine and 2'-deoxyguanosine. Synthesis of all stereoisomers, isomeric assignment, and biological activity.	2000 Mar 10	10814087
3'-azido-3'-deoxythimidine (AZT) is glucuronidated by human UDP-glucuronosyltransferase 2B7 (UGT2B7).	2000 May	10772627
Fetal mitochondrial heart and skeletal muscle damage in Erythrocebus patas monkeys exposed in utero to 3'-azido-3'-deoxythymidine.	2000 May 1	10791874
Anti-human immunodeficiency virus activity of novel aminoglycoside-arginine conjugates at early stages of infection.	2000 May 1	10791873
Anti-AIDS agents part 41: synthesis and anti-HIV activity of 3',4'-di-o-(-)-camphanoyl-(+)-cis-khellactone (DCK) lactam analogues.	2000 May 15	10843202

Patents

Sample Use Guides

In Vivo Use Guide

Treatment of HIV-1 infection: Adults: 600 mg/day in divided doses with other antiretroviral agents. Pediatric patients (6 weeks to <18 years of age): Dosage should be calculated based on body weight not to exceed adult dose.

Route of Administration: Oral

In Vitro Use Guide

The antiviral activity of CD8(+) cells from 2 LTSs was inhibited by 5 uM of zidovudine.

Substance Class	Chemical Created by `admin` on `Wed Apr 02 07:35:19 GMT 2025` Edited by `admin` on `Wed Apr 02 07:35:19 GMT 2025`
Record UNII	4B9XT59T7S
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

ZIDOVUDINE

Official Name

English

COMBIVIR COMPONENT ZIDOVUDINE

Preferred Name

English

ZIDOVUDINE [EP MONOGRAPH]

Common Name

English

BW-A509U

Code

English

AZIDOTHYMIDINE

Systematic Name

English

3'-DEOXY-3'-AZIDOTHYMIDINE

Systematic Name

English

THYMIDINE, 3'-AZIDO-3'-DEOXY-

Systematic Name

English

ZDV

Common Name

English

ZIDOVUDINE [MI]

Common Name

English

ZIDOVUDINE [USP-RS]

Common Name

English

ZIDOVUDINE [EP IMPURITY]

Common Name

English

AZT

Common Name

English

TRIZIVIR COMPONENT ZIDOVUDINE

Brand Name

English

ZIDOVUDINE [IARC]

Common Name

English

ZIDOVUDINE [USAN]

Common Name

English

ZIDOVUDINE [JAN]

Common Name

English

COMPOUND S

Code

English

ZIDOVUDINE [EMA EPAR]

Common Name

English

ZIDOVUDINE [ORANGE BOOK]

Common Name

English

ZIDOVUDINE [VANDF]

Common Name

English

RETROVIR

Brand Name

English

3'-AZIDO-3'-DEOXYTHYMIDINE

Systematic Name

English

ZIDOVUDINE [MART.]

Common Name

English

ZIDOVUDINE [USP MONOGRAPH]

Common Name

English

3'-AZT

Common Name

English

ZIDOVUDINE [WHO-IP]

Common Name

English

3'-AZIDOTHYMIDINE

Systematic Name

English

ZIDOVUDINE [HSDB]

Common Name

English

zidovudine [INN]

Common Name

English

BW-A-509U

Code

English

NSC-602670

Code

English

Zidovudine [WHO-DD]

Common Name

English

ZIDOVUDINUM [WHO-IP LATIN]

Common Name

English

LAMIVUDINE/ZIDOVUDINE TEVA COMPONENT ZIDOVUDINE

Brand Name

English

Classification Tree Code System Code

EMA ASSESSMENT REPORTS

COMBIVIR (AUTHORIZED: HIV INFECTIONS)