Product Information
Registration Status: ActiveSIN14544P
FOLOTYN SOLUTION FOR INFUSION 20MG/ML is approved to be sold in Singapore with effective from 2014-04-30. It is marketed by MUNDIPHARMA PHARMACEUTICALS PTE LTD, with the registration number of SIN14544P.
This product contains Pralatrexate 20mg/ml in the form of INFUSION, SOLUTION. It is approved for INTRAVENOUS use.
This product is manufactured by Baxter Oncology GmbH in GERMANY.
It is a Prescription Only Medicine that can only be obtained from a doctor or a dentist, or a pharmacist with a prescription from a Singapore-registered doctor or dentist.
Product Reference
Important Note: For generic product, the SPC/PIL provided may not be brand specific.
{{/items}} {{^items}}Description
Pralatrexate is an antimetabolite for the treatment of relapsed or refractory peripheral T-cell lymphoma. It is more efficiently retained in cancer cells than methotrexate. FDA approved on September 24, 2009.
Indication
Treatment of relapsed or refractory peripheral T-cell lymphoma.
Mechanism of Action
The selectivity of pralatrexate for cancer cells is based upon the observation that cancer cells generally have an overexpression of reduced folate carrier protein-1 (RTC-1) compared to normal somatic cells. This carrier protein allows the entrance of pralatrexate into the cell. Upon entering the cell, folypolyglutamate synthase FPGS catalyzes the polyglutamination of pralatrexate so that it is retained inside the cell. Once inside, pralatrexate competitively inhibits dihydrofolate reductase (DHFR) and thymidylate synthase. Subsequent depletion of thymidine monophosphate (TMP) occurs so that the cancer cell is unable to synthesize DNA and RNA. As a result, the cancer cell cannot proliferate and is forced to undergo apoptosis. Pralatrexate is more effective against cells that are actively dividing.
Pharmacokinetics
- Absorption
- Pralatrexate demonstrates linear pharmacokinetics with a multiphasic decline with both diasteromers over dose range of 30-325 mg/m^2. Bioavailability, nonformulated preparation = 13 - 20%
- Distribution
- Vss, R-pralatrexate = 37 L Vss, S-pralatrexate = 105 L
- Metabolism
- No involvement of CYP450 enzyme system or glucuronidases.
- Elimination
Clearance
R- pralatrexate = 191 mL/min S- pralatrexate = 417 mL/min Mean clearance of both enantiomers is 220 mL/min.
Toxicity
Mucositis is the dose-limiting toxicity. Folic acid and vitamin B12 supplements do not prevent mucositis from happening.
Active Ingredient/Synonyms
(2S)-2-((4-((1RS)-1-((2,4-diaminopteridin-6-yl)methyl)but-3-ynyl)benzoyl)amino)pentanedioic acid | (2S)-2-({4-[1-(2,4-diaminopteridin-6-yl)pent-4-yn-2-yl]benzoyl}amino)pentanedioic acid | 10-Propargyl-10-deazaaminopterin | N-(4-(1-((2,4-Diamino-6-pteridinyl)methyl)-3-butynyl)benzoyl)-L-glutamic acid | PDX | Pralatrexato | Pralatrexatum | Pralatrexate |
Source of information: Drugbank (External Link). Last updated on: 3rd July 18. *Trade Name used in the content below may not be the same as the HSA-registered product.