*** CHEMICAL IDENTIFICATION ***
RTECS NUMBER : XP2072000
CHEMICAL NAME : Thymidine, 3'-azido-3'-deoxy-
CAS REGISTRY NUMBER : 30516-87-1
LAST UPDATED : 199712
DATA ITEMS CITED : 36
MOLECULAR FORMULA : C10-H13-N5-O4
MOLECULAR WEIGHT : 267.28
COMPOUND DESCRIPTOR : Tumorigen
Drug
Mutagen
Reproductive Effector
Human
SYNONYMS/TRADE NAMES :
* 3'-Azido-3'-deoxythymidine
* Azidothymidine
* AZT
* BW-A 509U
* Retrovir
* Zidovudine
*** HEALTH HAZARD DATA ***
** ACUTE TOXICITY DATA **
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Human - woman
DOSE/DURATION : 1 gm/kg/6W-I
TOXIC EFFECTS :
Skin and Appendages - nails
REFERENCE :
AIMEAS Annals of Internal Medicine. (American College of Physicians, 4200
Pine St., Philadelphia, PA 19104) V.1- 1927- Volume(issue)/page/year:
107,350,1987
TYPE OF TEST : LDLo - Lowest published lethal dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Human - man
DOSE/DURATION : 86 mg/kg/1W-I
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold
Behavioral - headache
REFERENCE :
LANCAO Lancet. (7 Adam St., London WC2N 6AD, UK) V.1- 1823-
Volume(issue)/page/year: 2,1392,1986
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Human - man
DOSE/DURATION : 434 mg/kg/38D-I
TOXIC EFFECTS :
Blood - changes in cell count (unspecified)
Blood - aplastic anemia
Blood - changes in bone marrow (not otherwise specified)
REFERENCE :
AIMEAS Annals of Internal Medicine. (American College of Physicians, 4200
Pine St., Philadelphia, PA 19104) V.1- 1927- Volume(issue)/page/year:
107,502,1987
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Unreported
SPECIES OBSERVED : Human - man
DOSE/DURATION : 69 mg/kg
TOXIC EFFECTS :
Sense Organs and Special Senses (Eye) - retinal changes (pigmentary
depositions, retinitis, other)
REFERENCE :
AIMEAS Annals of Internal Medicine. (American College of Physicians, 4200
Pine St., Philadelphia, PA 19104) V.1- 1927- Volume(issue)/page/year:
114,297,1991
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - rat
DOSE/DURATION : 3084 mg/kg
TOXIC EFFECTS :
Sense Organs and Special Senses (Eye) - ptosis
Behavioral - somnolence (general depressed activity)
REFERENCE :
FAATDF Fundamental and Applied Toxicology. (Academic Press, Inc., 1 E.
First St., Duluth, MN 55802) V.1- 1981- Volume(issue)/page/year:
32,129,1996
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Intravenous
SPECIES OBSERVED : Rodent - rat
DOSE/DURATION : >70 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
USXXAM United States Patent Document. (U.S. Patent Office, Box 9,
Washington, DC 20231) Volume(issue)/page/year: #4804651
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Unreported
SPECIES OBSERVED : Rodent - rat
DOSE/DURATION : >750 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
USXXAM United States Patent Document. (U.S. Patent Office, Box 9,
Washington, DC 20231) Volume(issue)/page/year: #4857511
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - mouse
DOSE/DURATION : 3062 mg/kg
TOXIC EFFECTS :
Sense Organs and Special Senses (Eye) - ptosis
Behavioral - somnolence (general depressed activity)
REFERENCE :
FAATDF Fundamental and Applied Toxicology. (Academic Press, Inc., 1 E.
First St., Duluth, MN 55802) V.1- 1981- Volume(issue)/page/year:
32,129,1996
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Intravenous
SPECIES OBSERVED : Rodent - mouse
DOSE/DURATION : >70 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
USXXAM United States Patent Document. (U.S. Patent Office, Box 9,
Washington, DC 20231) Volume(issue)/page/year: #4804651
TYPE OF TEST : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE : Unreported
SPECIES OBSERVED : Rodent - mouse
DOSE/DURATION : >750 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
USXXAM United States Patent Document. (U.S. Patent Office, Box 9,
Washington, DC 20231) Volume(issue)/page/year: #4857511
** OTHER MULTIPLE DOSE TOXICITY DATA **
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - rat
DOSE/DURATION : 54600 mg/kg/1Y-I
TOXIC EFFECTS :
Blood - pigmented or nucleated red blood cells
Blood - changes in erythrocyte (RBC) count
REFERENCE :
FAATDF Fundamental and Applied Toxicology. (Academic Press, Inc., 1 E.
First St., Duluth, MN 55802) V.1- 1981- Volume(issue)/page/year:
32,129,1996
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - rat
DOSE/DURATION : 91 gm/kg/26W-I
TOXIC EFFECTS :
Blood - normocytic anemia
REFERENCE :
YKYUA6 Yakkyoku. Pharmacy. (Nanzando, 4-1-11, Yushima, Bunkyo-ku, Tokyo,
Japan) V.1- 1950- Volume(issue)/page/year: 39,595,1988
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - rat
DOSE/DURATION : 47 gm/kg/94D-I
TOXIC EFFECTS :
Blood - pigmented or nucleated red blood cells
Blood - changes in bone marrow (not otherwise specified)
Blood - changes in erythrocyte (RBC) count
REFERENCE :
FAATDF Fundamental and Applied Toxicology. (Academic Press, Inc., 1 E.
First St., Duluth, MN 55802) V.1- 1981- Volume(issue)/page/year:
17,159,1991
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - mouse
DOSE/DURATION : 4700 mg/kg/94D-I
TOXIC EFFECTS :
Blood - pigmented or nucleated red blood cells
Blood - changes in bone marrow (not otherwise specified)
Blood - changes in erythrocyte (RBC) count
REFERENCE :
FAATDF Fundamental and Applied Toxicology. (Academic Press, Inc., 1 E.
First St., Duluth, MN 55802) V.1- 1981- Volume(issue)/page/year:
17,159,1991
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - mouse
DOSE/DURATION : 14500 mg/kg/29D-I
TOXIC EFFECTS :
Blood - pigmented or nucleated red blood cells
Blood - changes in erythrocyte (RBC) count
Blood - changes in leukocyte (WBC) count
REFERENCE :
FAATDF Fundamental and Applied Toxicology. (Academic Press, Inc., 1 E.
First St., Duluth, MN 55802) V.1- 1981- Volume(issue)/page/year:
17,159,1991
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Intraperitoneal
SPECIES OBSERVED : Rodent - mouse
DOSE/DURATION : 6800 mg/kg/17D-I
TOXIC EFFECTS :
Kidney, Ureter, Bladder - changes in tubules (including acute renal failure,
acute tubular necrosis)
Blood - pigmented or nucleated red blood cells
Blood - changes in erythrocyte (RBC) count
REFERENCE :
TXAPA9 Toxicology and Applied Pharmacology. (Academic Press, Inc., 1 E.
First St., Duluth, MN 55802) V.1- 1959- Volume(issue)/page/year:
139,324,1996
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Mammal - dog
DOSE/DURATION : 7 gm/kg/2W-I
TOXIC EFFECTS :
Blood - leukopenia
Blood - thrombocytopenia
Nutritional and Gross Metabolic - weight loss or decreased weight gain
REFERENCE :
FAATDF Fundamental and Applied Toxicology. (Academic Press, Inc., 1 E.
First St., Duluth, MN 55802) V.1- 1981- Volume(issue)/page/year:
32,129,1996
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Primate - monkey
DOSE/DURATION : 3094 mg/kg/13W-I
TOXIC EFFECTS :
Blood - normocytic anemia
REFERENCE :
YKYUA6 Yakkyoku. Pharmacy. (Nanzando, 4-1-11, Yushima, Bunkyo-ku, Tokyo,
Japan) V.1- 1950- Volume(issue)/page/year: 39,595,1988
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Primate - monkey
DOSE/DURATION : 18200 mg/kg/26W-I
TOXIC EFFECTS :
Blood - pigmented or nucleated red blood cells
Blood - changes in other cell count (unspecified)
Blood - changes in erythrocyte (RBC) count
REFERENCE :
FAATDF Fundamental and Applied Toxicology. (Academic Press, Inc., 1 E.
First St., Duluth, MN 55802) V.1- 1981- Volume(issue)/page/year:
32,129,1996
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Primate - monkey
DOSE/DURATION : 12740 mg/kg/1Y-I
TOXIC EFFECTS :
Blood - pigmented or nucleated red blood cells
Blood - changes in erythrocyte (RBC) count
Blood - changes in platelet count
REFERENCE :
FAATDF Fundamental and Applied Toxicology. (Academic Press, Inc., 1 E.
First St., Duluth, MN 55802) V.1- 1981- Volume(issue)/page/year:
32,129,1996
** REPRODUCTIVE DATA **
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - rat
DOSE : 4200 mg/kg
SEX/DURATION : male 4 week(s) pre-mating
TOXIC EFFECTS :
Reproductive - Paternal Effects - prostate, seminal vesicle, Cowper's gland,
accessory glands
Reproductive - Paternal Effects - other effects on male
REFERENCE :
BCPCA6 Biochemical Pharmacology. (Pergamon Press Inc., Maxwell House,
Fairview Park, Elmsford, NY 10523) V.1- 1958- Volume(issue)/page/year:
42,1293,1991
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - rat
DOSE : 23 gm/kg
SEX/DURATION : male 85 day(s) pre-mating
female 26 day(s) pre-mating - 3 week(s) post-birth
TOXIC EFFECTS :
Reproductive - Fertility - post-implantation mortality (e.g. dead and/or
resorbed implants per total number of implants)
Reproductive - Fertility - litter size (e.g. # fetuses per litter; measured
before birth)
REFERENCE :
FAATDF Fundamental and Applied Toxicology. (Academic Press, Inc., 1 E.
First St., Duluth, MN 55802) V.1- 1981- Volume(issue)/page/year:
32,140,1996
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - rat
DOSE : 69 gm/kg
SEX/DURATION : male 85 day(s) pre-mating
female 26 day(s) pre-mating - 3 week(s) post-birth
TOXIC EFFECTS :
Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death,
e.g., stunted fetus)
Reproductive - Effects on Newborn - live birth index (measured after birth)
REFERENCE :
FAATDF Fundamental and Applied Toxicology. (Academic Press, Inc., 1 E.
First St., Duluth, MN 55802) V.1- 1981- Volume(issue)/page/year:
32,140,1996
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - rat
DOSE : 27900 mg/kg
SEX/DURATION : female 26 day(s) pre-mating - 15 day(s) post-birth
TOXIC EFFECTS :
Reproductive - Effects on Newborn - live birth index (measured after birth)
REFERENCE :
FAATDF Fundamental and Applied Toxicology. (Academic Press, Inc., 1 E.
First St., Duluth, MN 55802) V.1- 1981- Volume(issue)/page/year:
32,140,1996
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - mouse
DOSE : 910 mg/kg
SEX/DURATION : female 1-13 day(s) after conception
TOXIC EFFECTS :
Reproductive - Fertility - litter size (e.g. # fetuses per litter; measured
before birth)
Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death,
e.g., stunted fetus)
REFERENCE :
AMACCQ Antimicrobial Agents and Chemotherapy. (American Soc. for
Microbiology, 1913 I St., NW, Washington, DC 20006) V.1- 1972-
Volume(issue)/page/year: 36,2370,1992
TYPE OF TEST : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE : Oral
SPECIES OBSERVED : Rodent - rabbit
DOSE : 6500 mg/kg
SEX/DURATION : female 6-18 day(s) after conception
TOXIC EFFECTS :
Reproductive - Fertility - post-implantation mortality (e.g. dead and/or
resorbed implants per total number of implants)
REFERENCE :
FAATDF Fundamental and Applied Toxicology. (Academic Press, Inc., 1 E.
First St., Duluth, MN 55802) V.1- 1981- Volume(issue)/page/year:
32,140,1996
** MUTATION DATA **
TYPE OF TEST : Micronucleus test
TEST SYSTEM : Human Lymphocyte
DOSE/DURATION : 500 mg/L
REFERENCE :
MUREAV Mutation Research. (Elsevier Science Pub. B.V., POB 211, 1000 AE
Amsterdam, Netherlands) V.1- 1964- Volume(issue)/page/year: 321,113,1994
TYPE OF TEST : DNA inhibition
TEST SYSTEM : Human Lymphocyte
DOSE/DURATION : 10 umol/L
REFERENCE :
CNREA8 Cancer Research. (Public Ledger Building, Suit 816, 6th & Chestnut
Sts., Philadelphia, PA 19106) V.1- 1941- Volume(issue)/page/year:
49,5829,1989
TYPE OF TEST : Mutation test systems - not otherwise specified
TEST SYSTEM : Human Lymphocyte
DOSE/DURATION : 500 mg/L
REFERENCE :
MUREAV Mutation Research. (Elsevier Science Pub. B.V., POB 211, 1000 AE
Amsterdam, Netherlands) V.1- 1964- Volume(issue)/page/year: 321,113,1994
TYPE OF TEST : Cytogenetic analysis
TEST SYSTEM : Human Lymphocyte
DOSE/DURATION : 100 mg/L
REFERENCE :
MUREAV Mutation Research. (Elsevier Science Pub. B.V., POB 211, 1000 AE
Amsterdam, Netherlands) V.1- 1964- Volume(issue)/page/year: 321,113,1994
TYPE OF TEST : Sister chromatid exchange
TEST SYSTEM : Human Lymphocyte
DOSE/DURATION : 50 mg/L
REFERENCE :
MUREAV Mutation Research. (Elsevier Science Pub. B.V., POB 211, 1000 AE
Amsterdam, Netherlands) V.1- 1964- Volume(issue)/page/year: 321,113,1994
TYPE OF TEST : Micronucleus test
ROUTE OF EXPOSURE : Intraperitoneal
TEST SYSTEM : Rodent - mouse
DOSE/DURATION : 170 mg/kg/2W (Intermittent)
REFERENCE :
MUREAV Mutation Research. (Elsevier Science Pub. B.V., POB 211, 1000 AE
Amsterdam, Netherlands) V.1- 1964- Volume(issue)/page/year: 368,301,1996
TYPE OF TEST : Cytogenetic analysis
ROUTE OF EXPOSURE : Oral
TEST SYSTEM : Rodent - mouse
DOSE/DURATION : 600 mg/kg/3D (Continuous)
REFERENCE :
EMMUEG Environmental and Molecular Mutagenesis. (Alan R. Liss, Inc., 41 E.
11th St., New York, NY 10003) V.10- 1987- Volume(issue)/page/year:
18,168,1991
TYPE OF TEST : Cytogenetic analysis
TEST SYSTEM : Rodent - hamster Ovary
DOSE/DURATION : 1 gm/L
REFERENCE :
MUREAV Mutation Research. (Elsevier Science Pub. B.V., POB 211, 1000 AE
Amsterdam, Netherlands) V.1- 1964- Volume(issue)/page/year: 321,113,1994
TYPE OF TEST : Sister chromatid exchange
TEST SYSTEM : Rodent - hamster Ovary
DOSE/DURATION : 500 mg/L
REFERENCE :
MUREAV Mutation Research. (Elsevier Science Pub. B.V., POB 211, 1000 AE
Amsterdam, Netherlands) V.1- 1964- Volume(issue)/page/year: 321,113,1994
*** STATUS IN U.S. ***
NTP Carcinogenesis studies; test completed (post peer review), October 1997
*** END OF RECORD ***