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Melphalan
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DRUG INFO Melphalan
Drug Name:
Melphalan
Indication: Used to treat cancer of the ovaries and a certain type of cancer in the bone marrow
Pharmacology: Melphalan is an antineoplastic in the class of alkylating agents and is used to treat various forms of cancer. Alkylating agents are so named because of their ability to add alkyl groups to many electronegative groups under conditions present in cells. They stop tumor growth by cross-linking guanine bases in DNA double-helix strands - directly attacking DNA. This makes the strands unable to uncoil and separate. As this is necessary in DNA replication, the cells can no longer divide. In addition, these drugs add methyl or other alkyl groups onto molecules where they do not belong which in turn inhibits their correct utilization by base pairing and causes a miscoding of DNA. Alkylating agents are cell cycle-nonspecific. Alkylating agents work by three different mechanisms all of which achieve the same end result - disruption of DNA function and cell death.
Mechanism Of Action: Alkylating agents work by three different mechanisms: 1) attachment of alkyl groups to DNA bases, 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.
Drug Category: Antineoplastic Agents; ATC:L01AA03
Brand Names/Synonyms: 3025 C. B.; ALKERAN; AT-290; Alkeran; CB 3025; L-PAM; L-Phenylalanine Mustard; L-Sarcolysin; L-Sarcolysine; L-Sarkolysin; Levofalan; Melfalan; Melphalan; Mephalan; NSC 8806; NSC-8806; Phenylalanine Mustard; Phenylalanine Nitrogen Mustard; Sarcolysine; Sarkolysin
Dosage Forms: tablets, injection
Absorption: incomplete, variable, 25-89% post oral dose
Interactions: DRUG INTERACTIONS
There are no known drug/drug interactions with oral ALKERAN
Vaccinations with live organism vaccines are not recommended in immunocompromised
individuals
Nalidixic acid together with high-dose intravenous melphalan has caused deaths in
children due to haemorrhagic enterocolitis.
Impaired renal function has been described in bone marrow transplant patients who
were conditioned with high-dose intravenous melphalan and who subsequently received
cyclosporin to prevent graft-versus-host disease
Chemical IUPAC Name: 2-amino-3-[4-[bis(2-chloroethyl)amino]phenyl]-propanoicacid
Chemical Formula: C13H18Cl2N2O2
Half Life: 1.5 (+/-0.83) hours
Drug Type: Approved Drug
# Accession No: APRD00118
CAS Registry Number: 148-82-3
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Melphalan News (When available)
Superiority of Alkeran®, Thalidomid® Prednisone Regimen for ... Jan 5, 2006 Cancer Consultants (press release), Researchers from France have concluded that a Alkeran (melphalan), prednisone, Thalidomid (thalidomide) regimen was superior to a standard Alkeran-prednisone ...
Celgene Spikes on Drug Approval Dec 31, 2005 Business New Jersey (subscription), The decision gives Celgene a third drug to sell in the US, along with Thalomid and Alkeran, which are both used to treat the blood cancer multiple myeloma. ...
Celgene Corporation Reviews Recent Highlights and Outlines 2006 ... Jan 9, 2006 MSN Money ...performance was attributed to growing product revenue and profits supported by multiple product revenue streams including, THALOMID(R), ALKERAN(R), FOCALIN XR ...
High Response Rate with Velcade™, Thalomid® and Dexamethasone ... Jan 6, 2006 Cancer Consultants (press release), The optimal treatment of patients with multiple myeloma is rapidly evolving with the availability of high-dose Alkeran® (melphalan) (200 mg/m2) supported by ...
Revlimid approval brings year-end cheer to Celgene Jan 2, 2006 Pharma Times (subscription), Revlimid joins Celgene's two commercialized products, namely Thalomid (thalidomide) and Alkeran (melphalan) for the blood cancer multiple myeloma. ...
From a cause, a cure Jan 8, 2006 Boston Globe, ...first performed at Yale in the mid-1940s, on a patient with Hodgkin's disease, which regressed dramatically after treatment with nitrogen mustard, a related ...
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