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QuickView for Pentostatin (compound)
PubChem
| Name: | Pentostatin |
|---|---|
| PubChem Compound ID: | 40926 |
| Description: | A potent inhibitor of ADENOSINE DEAMINASE. The drug induces APOPTOSIS of LYMPHOCYTES, and is used in the treatment of many lymphoproliferative malignancies, particularly HAIRY CELL LEUKEMIA. It is also synergistic with some other antineoplastic agents and has immunosuppressive activity. |
| Molecular formula: | C11H16N4O4 |
| Molecular weight: | 268.269 g/mol |
| Synonyms: |
Imidazo(4,5-d)(1,3)diazepin-8-ol, 3-(2-deoxy-beta-D-erythro-pentofuranosyl)-3,6,7,8-tetrahydro-, (R)-; Nipent; YK-176; 2'-DCF; CL 67310465; Imidazo[4,5-d][1,3]diazepin-8-ol, 3- (2-deoxy-.beta.-D-erythro-pentofuranosyl)-3,6,7,8- tetrahydro-, (R)-; Imidazo[4,5-d][1,3]diazepin-8-ol, 3-(2-deoxy-.beta.-D-erythro-pentofuranosyl)-3,4,7,8-tetrahydro-, (R)-; Pentostatin [USAN:BAN:INN:JAN]; 69196-00-5; (R)-Deoxycoformycin.
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DrugBank
Identification
| Name: | Pentostatin |
|---|---|
| Name (isomeric): | DB00552 |
| Drug Type: | small molecule |
| Description: | A potent inhibitor of ADENOSINE DEAMINASE. The drug induces APOPTOSIS of LYMPHOCYTES, and is used in the treatment of many lymphoproliferative malignancies, particularly HAIRY CELL LEUKEMIA. It is also synergistic with some other antineoplastic agents and has immunosuppressive activity. |
| Synonyms: |
2'-DCF; Deoxycoformycin; 2'-Dexoycoformycin; 2'-Deoxycoformycin
|
| Brand: | Co-V, Vidarbine, Vira a Deaminase Inhibitor, Covidarabine, Nipent, Co-Vidarabine, PD-ADI |
| Category: | Antineoplastic Agents, Antibiotics, Enzyme Inhibitors, Immunosuppressive Agents |
| CAS number: | 53910-25-1 |
Pharmacology
| Indication: | For the treatment of hairy cell leukaemia refractory to alpha interferon. |
|---|---|
| Pharmacology: |
Pentostatin is an antineoplastic anti-metabolite used in the treatment of several forms of leukemia including acute nonlymphocytic leukemia and hairy cell leukemia. Anti-metabolites masquerade as purine or pyrimidine - which become the building blocks of DNA. They prevent these substances becoming incorporated in to DNA during the "S" phase (of the...
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| Mechanism of Action: |
Pentostatin is a potent transition state inhibitor of adenosine deaminase (ADA), the greatest activity of which is found in cells of the lymphoid system. T-cells have higher ADA activity than B-cells, and T-cell malignancies have higher activity than B-cell malignancies. The cytotoxicity that results from prevention of catabolism of adenosine or de...
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| Absorption: | Not absorbed orally, crosses blood brain barrier. |
| Protein binding: | 4% |
| Biotransformation: | Primarily hepatic, but only small amounts are metabolized. |
| Route of elimination: | In man, following a single dose of 4 mg/m2 of pentostatin infused over 5 minutes, approximately 90% of the dose was excreted in the urine as unchanged pentostatin and/or metabolites as measured by adenosine deaminase inhibitory activity. |
| Half Life: | 5.7 hours (with a range between 2.6 and 16 hrs) |
| Clearance: | 68 mL/min/m2 |
| Toxicity: | LD50=128 mg/kg (mouse), side effects include lethargy, rash, fatigue, nausea and myelosuppression. |
| Affected organisms: | Humans and other mammals |
Interactions
| Drug interaction: |
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Targets
