ALKERAN- melphalan tablet, film coated

국가: 미국

언어: 영어

출처: NLM (National Library of Medicine)

유효 성분:

MELPHALAN (UNII: Q41OR9510P) (MELPHALAN - UNII:Q41OR9510P)

제공처:

ApoPharma USA, Inc.

INN (국제 이름):

MELPHALAN

구성:

MELPHALAN 2 mg

관리 경로:

ORAL

처방전 유형:

PRESCRIPTION DRUG

치료 징후:

ALKERAN Tablets are indicated for the palliative treatment of multiple myeloma and for the palliation of non-resectable epithelial carcinoma of the ovary. ALKERAN should not be used in patients whose disease has demonstrated a prior resistance to this agent. Patients who have demonstrated hypersensitivity to melphalan should not be given the drug.

제품 요약:

ALKERAN is supplied as white, film-coated, round, biconvex tablets containing 2 mg melphalan in amber glass bottles with child-resistant closures. One side is engraved with “GX EH3” and the other side is engraved with an “A.” Bottle of 50 (NDC 52609-0001-5). Store in a refrigerator, 2° to 8°C (36° to 46°F). Protect from light.

승인 상태:

New Drug Application

제품 특성 요약

ALKERAN- MELPHALAN TABLET, FILM COATED
APOPHARMA USA, INC.
----------
ALKERAN
(MELPHALAN)
TABLETS
WARNING
ALKERAN (melphalan) should be administered under the supervision of a
qualified
physician experienced in the use of cancer chemotherapeutic agents.
Severe bone
marrow suppression with resulting infection or bleeding may occur.
Melphalan is
leukemogenic in humans.
Melphalan produces chromosomal aberrations in vitro and in vivo and,
therefore,
should be considered potentially mutagenic in humans.
DESCRIPTION
ALKERAN (melphalan), also known as L-phenylalanine mustard,
phenylalanine mustard,
L-PAM, or L-sarcolysin, is a phenylalanine derivative of nitrogen
mustard. Melphalan is a
bifunctional alkylating agent which is active against selective human
neoplastic diseases.
It is known chemically as
4-[bis(2-chloroethyl)amino]-_L-_phenylalanine. The molecular
formula is C
H
Cl
N O and the molecular weight is 305.20. The structural formula is:
Melphalan is the active L-isomer of the compound and was first
synthesized in 1953 by
Bergel and Stock; the D-isomer, known as medphalan, is less active
against certain
animal tumors, and the dose needed to produce effects on chromosomes
is larger than
that required with the L-isomer. The racemic (DL−) form is known as
merphalan or
sarcolysin.
Melphalan is practically insoluble in water and has a pKa of ~2.5.
ALKERAN (melphalan) is available in tablet form for oral
administration. Each film-coated
tablet contains 2 mg melphalan and the inactive ingredients colloidal
silicon dioxide,
crospovidone, hypromellose, macrogol/PEG 400, magnesium stearate,
microcrystalline
cellulose, and titanium dioxide.
CLINICAL PHARMACOLOGY
Melphalan is an alkylating agent of the bischloroethylamine type. As a
result, its
®
13
18
2
2
2
1
cytotoxicity appears to be related to the extent of its interstrand
cross-linking with DNA,
probably by binding at the N position of guanine. Like other
bifunctional alkylating
agents, it is active against both resting and rapidly dividing tumor
cells.
PHARMACOKINET