Product Information
Registration Status: ActiveALKERAN TABLET 2mg (REVISED FORMULA) is approved to be sold in Singapore with effective from 2002-02-26. It is marketed by DCH AURIGA SINGAPORE, with the registration number of SIN11822P.
This product contains Melphalan 2mg in the form of TABLET, FILM-COATED. It is approved for ORAL use.
This product is manufactured by Excella 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.
Description
An alkylating nitrogen mustard that is used as an antineoplastic in the form of the levo isomer - melphalan, the racemic mixture - merphalan, and the dextro isomer - medphalan; toxic to bone marrow, but little vesicant action; potential carcinogen. [PubChem]
Indication
For the palliative treatment of multiple myeloma and for the palliation of non-resectable epithelial carcinoma of the ovary. Has also been used alone or as part of various chemotherapeutic regimens as an adjunct to surgery in the treatment of breast cancer, alone or in combination regimens for palliative treatment of locally recurrent or unresectable in-transit metastatic melanoma of the extremities, as well as for the treatment of amyloidosis with prednisone.
Mechanism of Action
Alkylating agents work by three different mechanisms: 1) attachment of alkyl groups to DNA bases (primarily at the N-7 position of guanine and to a lesser extent, at the N-3 position of adenine), forming monoadducts and resulting in the DNA being fragmented by repair enzymes in their attempts to replace the alkylated bases, preventing DNA synthesis and RNA transcription from the affected DNA, 2) DNA damage via the formation of cross-links (bonds between atoms in the DNA) which prevents DNA from being separated for synthesis or transcription, and 3) the induction of mispairing of the nucleotides leading to mutations.
Pharmacokinetics
- Absorption
- Incomplete, variable, 25-89% post oral dose
- Distribution
- * 0.5 L/kg
- Metabolism
- Melphalan is not actively metabolised, it spontaneously degrades to mono and dihydroxy products.
- Elimination
Toxicity
Vomiting, ulceration of the mouth, diarrhea, and hemorrhage of the gastrointestinal tract; The principal toxic effect is bone marrow suppression. LD50=11.2 mg/kg (orally in rat)
Active Ingredient/Synonyms
3-(P-(Bis(2-chloroethyl)amino)phenyl)-L-alanine | 3-P-(Di(2-chloroethyl)amino)-phenyl-L-alanine | 4-(Bis(2-chloroethyl)amino)-L-phenylalanine | L-3-(P-(Bis(2-chloroethyl)amino)phenyl)alanine | L-PAM | L-Phenylalanine mustard | L-Sarcolysine | Melfalano | Melphalanum | p-Bis(beta-chloroethyl)aminophenylalanine | P-Di-(2-chloroethyl)amino-L-phenylalanine | P-L-Sarcolysin | P-N-Bis(2-chloroethyl)amino-L-phenylalanine | p-N,N-bis(2-chloroethyl)amino-L-phenylalanine | Phenylalanine mustard | Phenylalanine nitrogen mustard | Melphalan |
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.