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| Primary information |
|---|
| ID | 10142 |
| Therapeutic ID | Th1020 |
| Protein Name | Asparaginase |
| Sequence | >Th1020_Asparaginase
MEFFKKTALAALVMGFSGAALALPNITILATGGTIAGGGDSATKSNYTVGKVGVENLVNAVPQLKDIANVKGEQVVNIGSQDMNDNVWLTLAKKINTDCDKTDGFVITHGTDTMEETAYFLDLTVKCDKPVVMVGAMRPSTSMSADGPFNLYNAVVTAADKASANRGVLVVMNDTVLDGRDVTKTNTTDVATFKSVNYGPLGYIHNGKIDYQRTPARKHTSDTPFDVSKLNELPKVGIVYNYANASDLPAKALVDAGYDGIVSAGVGNGNLYKSVFDTLATAAKTGTAVVRSSRVPTGATTQDAEVDDAKYGFVASGTLNPQKARVLLQLALTQTKDPQQIQQIFNQY
|
| Molecular Weight | 31731.9 |
| Chemical Formula | C1377H2208N382O442S17 |
| Isoelectric Point | 4.67 |
| Hydrophobicity | 0.059 |
| Melting point | NA |
| Half-life | 8-30 hours |
| Description | L-asparagine amidohydrolase from E. coli |
| Indication/Disease | To treat acute lympocytic leukemia and non-Hodgkins lymphoma |
| Pharmacodynamics | In most patients with acute leukemia, the malignant cells are dependent on an exogenous source of asparagine for survival. Normal cells, however, are able to synthesize asparagine and thus are affected less by the rapid depletion produced by treatment with the enzyme asparaginase. Elspar exploits a metabolic defect in asparagine synthesis of some malignant cells. |
| Mechanism of Action | Asparaginase converts asparagine to aspartic acid and ammonia. It facilitates production of oxalo-acetate which is needed for general cellular metabolism. Some malignant cells lose the ability to produce asparagine and thus the loss of exogenous sources of asparagine leads to cell death. |
| Toxicity | NA |
| Metabolism | NA |
| Absorption | NA |
| Apparent volume of distribution was slightly greater than the plasma volume. Asparaginase levels in cerebrospinal fluid were less than 1% of concurrent plasma levels |
| Clearance | NA |
| Categories | Amidohydrolases, Antineoplastic Agents, Antineoplastic and Immunomodulating Agents, Asparaginase, Asparagine-specific Enzyme, Enzymes, Enzymes and Coenzymes, Hydrolases, Narrow Therapeutic Index Drugs, Thyroxine-binding globulin inhibitors |
| Patents Number | NA |
| Date of Issue | NA |
| Date of Expiry | NA |
| Drug Interaction | Trastuzumab may increase the risk of neutropenia and anemia. Monitor closely for signs and symptoms of adverse events. |
| Target | L-asparagine |
| Brand Name | Elspar |
| Company | Lundbeck Inc. |
| Brand Description | Lundbeck Inc. |
| Prescribed For | To treat acute lymphocytic leukemia. It is used along with other cancer medicines. Elspar is an antineoplastic agent that works by decreasing the amount of asparagine in the body, which kills certain leukemia cells |
| Chemical Name | NA |
| Formulation | Each vial contains 10,000 International Units of asparaginase and 80 mg of mannitol. |
| Physical Appearance | Lyophilized plug or powder |
| Route of Administration | Intravenous or intramuSubcutaneousular. Intravenou |
| Recommended Dosage | The recommended dose of Elspar is 6,000 International Units/m_ intramuscularly (IM) or intravenously (IV) three times a week. |
| Contraindication | Allergic |
| Side Effects | Fever, chills (see flu like symptoms), Nausea and vomiting, Allergic reaction, (sudden onset of wheezing, itching, rash, face swelling, agitation, low blood pressure). You will be monitored closely for this reaction, Poor appetite, Stomach cramping |
| Useful Link 1 | Link |
| Useful Link 2 | NA |
| Remarks | NA |