*** CHEMICAL IDENTIFICATION ***

RTECS NUMBER            : VJ6700000
CHEMICAL NAME           : Rifamycin XIV,
                          1,4-dihydro-1-deoxy-1',4-didehydro-5'-(2-methylpropyl
                          )-1-oxo-
CAS REGISTRY NUMBER     : 72559-06-9
BEILSTEIN REFERENCE NO. : 3584778
LAST UPDATED            : 199709
DATA ITEMS CITED        : 11
MOLECULAR FORMULA       : C46-H62-N4-O11
MOLECULAR WEIGHT        : 847.12
COMPOUND DESCRIPTOR     : Drug
                          Human
SYNONYMS/TRADE NAMES :
   * Antibiotic LM 427
   *   4-Deoxo-3,4-(2-spiro(N-isobutyl-4-piperidyl)-2,5-dihydro-1H-imidazo)-rif
     amycin S
   * 1,4-Dihydro-1-deoxy-1',4-didehydro-5'-(2-methylpropyl)-1-oxorifamycin XIV
   * LM 427
   * Rifabutin
   * Rifabutine
 
                       *** HEALTH HAZARD DATA ***
 
                        ** ACUTE TOXICITY DATA **
 
TYPE OF TEST            : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE       : Unreported
SPECIES OBSERVED        : Human - man
DOSE/DURATION           : 60 mg/kg/14D-I
TOXIC EFFECTS :
   Blood - agranulocytosis
REFERENCE :
   LANCAO Lancet.  (7 Adam St., London WC2N 6AD, UK)  V.1-    1823-
   Volume(issue)/page/year: 348,685,1996
 
TYPE OF TEST            : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE       : Unreported
SPECIES OBSERVED        : Human - woman
DOSE/DURATION           : 84 mg/kg/14D-I
TOXIC EFFECTS :
   Blood - agranulocytosis
REFERENCE :
   LANCAO Lancet.  (7 Adam St., London WC2N 6AD, UK)  V.1-    1823-
   Volume(issue)/page/year: 348,685,1996
 
TYPE OF TEST            : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Rodent - rat
DOSE/DURATION           : >5 gm/kg
TOXIC EFFECTS :
   Behavioral - somnolence (general depressed activity)
REFERENCE :
   ETPAEK Experimental and Toxicologic Pathology.  (Gustav Fischer Verlag Jena,
   Postfach 100537, D-07705 Jena, Germany)  V.44-    1992-
   Volume(issue)/page/year: 47,1,1995
 
TYPE OF TEST            : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE       : Intravenous
SPECIES OBSERVED        : Rodent - rat
DOSE/DURATION           : 51 mg/kg
TOXIC EFFECTS :
   Behavioral - somnolence (general depressed activity)
   Behavioral - convulsions or effect on seizure threshold
   Lungs, Thorax, or Respiration - dyspnea
REFERENCE :
   ETPAEK Experimental and Toxicologic Pathology.  (Gustav Fischer Verlag Jena,
   Postfach 100537, D-07705 Jena, Germany)  V.44-    1992-
   Volume(issue)/page/year: 47,1,1995
 
TYPE OF TEST            : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Rodent - mouse
DOSE/DURATION           : 3322 mg/kg
TOXIC EFFECTS :
   Behavioral - somnolence (general depressed activity)
REFERENCE :
   ETPAEK Experimental and Toxicologic Pathology.  (Gustav Fischer Verlag Jena,
   Postfach 100537, D-07705 Jena, Germany)  V.44-    1992-
   Volume(issue)/page/year: 47,1,1995
 
TYPE OF TEST            : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE       : Intravenous
SPECIES OBSERVED        : Rodent - mouse
DOSE/DURATION           : 266 mg/kg
TOXIC EFFECTS :
   Behavioral - somnolence (general depressed activity)
   Behavioral - ataxia
   Lungs, Thorax, or Respiration - dyspnea
REFERENCE :
   ETPAEK Experimental and Toxicologic Pathology.  (Gustav Fischer Verlag Jena,
   Postfach 100537, D-07705 Jena, Germany)  V.44-    1992-
   Volume(issue)/page/year: 47,1,1995
 
TYPE OF TEST            : LD - Lethal dose
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Mammal - dog
DOSE/DURATION           : >2 gm/kg
TOXIC EFFECTS :
   Details of toxic effects not reported other than lethal dose value
REFERENCE :
   ETPAEK Experimental and Toxicologic Pathology.  (Gustav Fischer Verlag Jena,
   Postfach 100537, D-07705 Jena, Germany)  V.44-    1992-
   Volume(issue)/page/year: 47,1,1995
 
TYPE OF TEST            : LD - Lethal dose
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Primate - monkey
DOSE/DURATION           : >4 gm/kg
TOXIC EFFECTS :
   Details of toxic effects not reported other than lethal dose value
REFERENCE :
   ETPAEK Experimental and Toxicologic Pathology.  (Gustav Fischer Verlag Jena,
   Postfach 100537, D-07705 Jena, Germany)  V.44-    1992-
   Volume(issue)/page/year: 47,1,1995
 
                 ** OTHER MULTIPLE DOSE TOXICITY DATA **
 
TYPE OF TEST            : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Rodent - rat
DOSE/DURATION           : 9100 mg/kg/13W-C
TOXIC EFFECTS :
   Liver - other changes
   Kidney, Ureter, Bladder - other changes
   Blood - changes in spleen
REFERENCE :
   ETPAEK Experimental and Toxicologic Pathology.  (Gustav Fischer Verlag Jena,
   Postfach 100537, D-07705 Jena, Germany)  V.44-    1992-
   Volume(issue)/page/year: 47,1,1995
 
TYPE OF TEST            : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Rodent - rat
DOSE/DURATION           : 29120 mg/kg/1Y-I
TOXIC EFFECTS :
   Blood - normocytic anemia
   Endocrine - changes in spleen weight
   Biochemical - Enzyme inhibition, induction, or change in blood or tissue
   levels - transaminases
REFERENCE :
   ETPAEK Experimental and Toxicologic Pathology.  (Gustav Fischer Verlag Jena,
   Postfach 100537, D-07705 Jena, Germany)  V.44-    1992-
   Volume(issue)/page/year: 47,1,1995
 
TYPE OF TEST            : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Rodent - mouse
DOSE/DURATION           : 47 mg/kg/1Y-C
TOXIC EFFECTS :
   Blood - normocytic anemia
   Blood - changes in spleen
   Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol)
REFERENCE :
   ETPAEK Experimental and Toxicologic Pathology.  (Gustav Fischer Verlag Jena,
   Postfach 100537, D-07705 Jena, Germany)  V.44-    1992-
   Volume(issue)/page/year: 47,1,1995
 
                            *** END OF RECORD ***