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Drug

D1368 | oxaliplatin

Molecular Formula C8H12N2O4Pt
Molecular Weight 395.3
Structure
State solid
Clearance * 10 - 17 L/h [renal clearance]
Volume of distribution * 440 L [single 2-hour IV infusion at dose of 85 mg/m^2] At the end of a 2-hour infusion of oxaliplatin, approximately 15% of the administered platinum is present in the systemic circulation. The remaining 85% is rapidly distributed into tissues or eliminated in the urine.
Route of elimination The major route of platinum elimination is renal excretion. At five days after a single 2-hour infusion of oxaliplatin, urinary elimination accounted for about 54% of the platinum eliminated, with fecal excretion accounting for only about 2%.
Protein binding Plasma protein binding of platinum (active metabolite) is irreversible and is greater than 90%, primarily to albumin and gamma-globulins. It is also irreversibly binds to erythrocytes.
Half life The decline of ultrafilterable platinum levels following oxaliplatin administartion is triphasic, with two distribution phases: t1/2alpha; 0.43 hours and t1/2beta; 16.8 hours. This is followed by a long terminal elimination phase that lasts 391 hours (t1/2gamma).
Absorption Bioavailability is complete following intravenous administration. When a single 2-hour intravenous infusion of oxaliplatin at a dose of 85 mg/m^2 is given, the peak serum concentration was 0.814 mcg/mL.
Trade names Eloxatin
Description blocking the duplication of DNA; Anti-cancer

L

L01XA03 Oxaliplatin


[L01XA] Platinum compounds


[L01X] OTHER ANTINEOPLASTIC AGENTS


[L01] ANTINEOPLASTIC AGENTS


[L] Antineoplastic and immunomodulating agents

Toxicity Dose Time Species Model Method Action Positive criterion Reference
APOPTOSIS 262

Organism Test type Route Dose (normalized dose) Effect Source
mouse LD50 intravenous 30mg/kg (30mg/kg) Cancer Treatment Reports. Vol. 61, Pg. 1519, 1977.
mouse LD50 intraperitoneal 19800ug/kg (19.8mg/kg) Rinsho Yakuri. Clinical Pharmacology. Vol. 16, Pg. 147, 1985.


  • (SP-4-2)-[(1R,2R)-Cyclohexane-1,2-diamine-?N,?N?][ethanedioato(2-)-?O1,?O2]platinum ACT 078 CCRIS 9143
    Lipoxal NCI60_002138 NSC 271670
    Oxalato(1,2-diaminocyclohexane)platinum(II) Oxaliplatin [USAN:USP:INN:BAN] Oxalitin
    Oxaloplatine Oxaloplatino Platinum (II), (cyclohexane-1,2-diammine)oxalato-
    Platinum, (1,2-cyclohexanediamine-N,N')(ethanedioato(2-)-O,O')-, (SP-4-2-(trans))- Platinum, (1,2-cyclohexanediamine-kappaN,kappaN')(ethanedioato(2-)-kappaO1,kappaO2)-, (SP-4-2-(trans))- [(1R,2R)-Cyclohexane-1,2-diaminato(2-)-kappa~2~N,N'][ethanedioato(2-)-kappa~2~O~1~,O~2~]platinum

    DrugBank DB00526
    CAS Number 61825-94-3, 63121-00-6
    PubChem Compound 43805