Peringatan Keamanan

The oral and intraperitoneal LD50 in rats is 4484 µg/kg and 11200 µg/kg, respectively. The subcutaneous LD50 in mice is 32 mg/kg.L47900

Overdoses resulting in death have been reported with melphalan. Overdoses, including intravenous doses up to 290 mg/m2 and oral doses up to 50 mg/day for 16 days, have been reported. Symptoms of overdose include severe nausea and vomiting, decreased consciousness, convulsions, muscular paralysis, cholinomimetic effects, mucositis, stomatitis, colitis, diarrhea, and hemorrhage of the gastrointestinal tract. Elevations in liver enzymes and veno-occlusive disease occur infrequently. Significant hyponatremia, caused by an associated inappropriate secretion of ADH syndrome, has been observed. Nephrotoxicity and adult respiratory distress syndrome have been reported rarely. The principal toxic effect is bone marrow suppression. Melphalan is not removed from plasma via hemodialysis, and overdose is typically managed by general supportive measures, with appropriate blood transfusions and antibiotics.L40928, L47890

Melphalan

DB01042

small molecule approved

Deskripsi

Melphalan is a nitrogen mustard or bischloroethylamine type alkylating agent.L40928 It was first synthesized in the early 1950s by substituting L-phenylalanine for the methyl group on nitrogen mustard.A261150, A261155 Melphalan is used in the treatment of multiple myeloma and ovarian carcinoma.L40928 It is also used for high-conditioning before hematopoietic stem cell transplant.L47890 It is also used to treat uveal melanoma with unresectable hepatic metastases.L47895

Struktur Molekul 2D

Berat 305.2
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) In patients given a single oral dose of 0.6 mg/kg of melphalan, the terminal elimination plasma half-life (± SD) was 1.5 ± 0.83 hours.[L40928] Following intravenous administration, the terminal elimination half-life is approximately 75 minutes.[L47890]
Volume Distribusi The volume of distribution of melphalan ranges from approximately 35.5 to 185.7 L/m<sup>2</sup>.[L47890] Penetration into cerebrospinal fluid is low.[L40928]
Klirens (Clearance) Average total body clearance (CL) ranges from approximately 250 to 325 mL/min/m<sup>2</sup>.[L47890]

Absorpsi

The absorption of oral melphalan is highly variable concerning both the time to the first appearance of the drug in plasma (range: 0 to 6 hours) and peak plasma concentration (Cmax). The average absolute bioavailability of melphalan ranges from 56% to 93%. High variability in bioavailability may be due to incomplete intestinal absorption, variable first-pass hepatic metabolism, or rapid hydrolysis. Tmax was one hour in patients who received single oral doses of 0.2 mg/kg to 0.25 mg/kg of melphalan. Oral administration of melphalan with a high-fat meal may reduce melphalan exposure (AUC) by 36% to 54%.L40928 Mean (± SD) Cmax and AUC0-inf were 5.8 ± 1.5 mcg/mL and 451 ± 109 mcg x min/mL, respectively, following intravenous administration of 100 mg/m2 in multiple myeloma patients.L47890

Metabolisme

Melphalan primarily undergoes chemical hydrolysis to inactive metabolites, monohydroxymelphalan and dihydroxymelphalan.L40928, L47890 No other melphalan metabolites have been observed in humans.L40928

Rute Eliminasi

About 5.8% to 21.3% of melphalan is excreted in urine.L47890

Interaksi Obat

527 Data
Denosumab The risk or severity of adverse effects can be increased when Denosumab is combined with Melphalan.
Etanercept The risk or severity of adverse effects can be increased when Etanercept is combined with Melphalan.
Peginterferon alfa-2a The risk or severity of adverse effects can be increased when Peginterferon alfa-2a is combined with Melphalan.
Interferon alfa-n1 The risk or severity of adverse effects can be increased when Interferon alfa-n1 is combined with Melphalan.
Interferon alfa-n3 The risk or severity of adverse effects can be increased when Interferon alfa-n3 is combined with Melphalan.
Peginterferon alfa-2b The risk or severity of adverse effects can be increased when Peginterferon alfa-2b is combined with Melphalan.
Anakinra The risk or severity of adverse effects can be increased when Anakinra is combined with Melphalan.
Interferon gamma-1b The risk or severity of adverse effects can be increased when Interferon gamma-1b is combined with Melphalan.
Interferon alfa-2a The risk or severity of adverse effects can be increased when Interferon alfa-2a is combined with Melphalan.
Aldesleukin The risk or severity of adverse effects can be increased when Aldesleukin is combined with Melphalan.
Adalimumab The risk or severity of adverse effects can be increased when Adalimumab is combined with Melphalan.
Gemtuzumab ozogamicin The risk or severity of adverse effects can be increased when Gemtuzumab ozogamicin is combined with Melphalan.
Pegaspargase The risk or severity of adverse effects can be increased when Pegaspargase is combined with Melphalan.
Infliximab The risk or severity of adverse effects can be increased when Infliximab is combined with Melphalan.
Interferon beta-1b The risk or severity of adverse effects can be increased when Interferon beta-1b is combined with Melphalan.
Interferon alfacon-1 The risk or severity of adverse effects can be increased when Interferon alfacon-1 is combined with Melphalan.
Rituximab The risk or severity of adverse effects can be increased when Rituximab is combined with Melphalan.
Basiliximab The risk or severity of adverse effects can be increased when Basiliximab is combined with Melphalan.
Muromonab The risk or severity of adverse effects can be increased when Muromonab is combined with Melphalan.
Ibritumomab tiuxetan The risk or severity of adverse effects can be increased when Ibritumomab tiuxetan is combined with Melphalan.
Tositumomab The risk or severity of adverse effects can be increased when Tositumomab is combined with Melphalan.
Alemtuzumab The risk or severity of adverse effects can be increased when Alemtuzumab is combined with Melphalan.
Alefacept The risk or severity of adverse effects can be increased when Alefacept is combined with Melphalan.
Efalizumab The risk or severity of adverse effects can be increased when Efalizumab is combined with Melphalan.
Antithymocyte immunoglobulin (rabbit) The risk or severity of adverse effects can be increased when Antithymocyte immunoglobulin (rabbit) is combined with Melphalan.
Interferon alfa-2b The risk or severity of adverse effects can be increased when Interferon alfa-2b is combined with Melphalan.
Daclizumab The risk or severity of adverse effects can be increased when Daclizumab is combined with Melphalan.
Phenylalanine The risk or severity of adverse effects can be increased when Phenylalanine is combined with Melphalan.
Flunisolide The risk or severity of adverse effects can be increased when Flunisolide is combined with Melphalan.
Bortezomib The risk or severity of adverse effects can be increased when Bortezomib is combined with Melphalan.
Cladribine Melphalan may increase the immunosuppressive activities of Cladribine.
Amsacrine The risk or severity of adverse effects can be increased when Amsacrine is combined with Melphalan.
Bleomycin The risk or severity of adverse effects can be increased when Bleomycin is combined with Melphalan.
Chlorambucil The risk or severity of adverse effects can be increased when Chlorambucil is combined with Melphalan.
Raltitrexed The risk or severity of adverse effects can be increased when Raltitrexed is combined with Melphalan.
Mitomycin The risk or severity of adverse effects can be increased when Mitomycin is combined with Melphalan.
Bexarotene The risk or severity of adverse effects can be increased when Bexarotene is combined with Melphalan.
Vindesine The risk or severity of adverse effects can be increased when Vindesine is combined with Melphalan.
Floxuridine The risk or severity of adverse effects can be increased when Floxuridine is combined with Melphalan.
Indomethacin The risk or severity of adverse effects can be increased when Indomethacin is combined with Melphalan.
Tioguanine The risk or severity of adverse effects can be increased when Tioguanine is combined with Melphalan.
Vinorelbine The risk or severity of adverse effects can be increased when Vinorelbine is combined with Melphalan.
Dexrazoxane The risk or severity of adverse effects can be increased when Dexrazoxane is combined with Melphalan.
Beclomethasone dipropionate The risk or severity of adverse effects can be increased when Beclomethasone dipropionate is combined with Melphalan.
Sorafenib The risk or severity of adverse effects can be increased when Sorafenib is combined with Melphalan.
Streptozocin The risk or severity of adverse effects can be increased when Streptozocin is combined with Melphalan.
Trifluridine The risk or severity of adverse effects can be increased when Trifluridine is combined with Melphalan.
Gemcitabine The risk or severity of adverse effects can be increased when Gemcitabine is combined with Melphalan.
Betamethasone The risk or severity of adverse effects can be increased when Betamethasone is combined with Melphalan.
Teniposide The risk or severity of adverse effects can be increased when Teniposide is combined with Melphalan.
Epirubicin The risk or severity of adverse effects can be increased when Epirubicin is combined with Melphalan.
Chloramphenicol The risk or severity of adverse effects can be increased when Chloramphenicol is combined with Melphalan.
Lenalidomide The risk or severity of adverse effects can be increased when Lenalidomide is combined with Melphalan.
Altretamine The risk or severity of adverse effects can be increased when Altretamine is combined with Melphalan.
Zidovudine The risk or severity of adverse effects can be increased when Zidovudine is combined with Melphalan.
Cisplatin The risk or severity of adverse effects can be increased when Cisplatin is combined with Melphalan.
Oxaliplatin The risk or severity of adverse effects can be increased when Oxaliplatin is combined with Melphalan.
Cyclophosphamide The risk or severity of adverse effects can be increased when Cyclophosphamide is combined with Melphalan.
Vincristine The risk or severity of adverse effects can be increased when Vincristine is combined with Melphalan.
Fluorouracil The risk or severity of adverse effects can be increased when Fluorouracil is combined with Melphalan.
Propylthiouracil The risk or severity of adverse effects can be increased when Propylthiouracil is combined with Melphalan.
Pentostatin The risk or severity of adverse effects can be increased when Pentostatin is combined with Melphalan.
Methotrexate The risk or severity of adverse effects can be increased when Methotrexate is combined with Melphalan.
Carbamazepine The risk or severity of adverse effects can be increased when Carbamazepine is combined with Melphalan.
Vinblastine The risk or severity of adverse effects can be increased when Vinblastine is combined with Melphalan.
Fluticasone propionate The risk or severity of adverse effects can be increased when Fluticasone propionate is combined with Melphalan.
Fluocinolone acetonide The risk or severity of adverse effects can be increased when Fluocinolone acetonide is combined with Melphalan.
Linezolid The risk or severity of adverse effects can be increased when Linezolid is combined with Melphalan.
Imatinib The risk or severity of adverse effects can be increased when Imatinib is combined with Melphalan.
Triamcinolone The risk or severity of adverse effects can be increased when Triamcinolone is combined with Melphalan.
Clofarabine The risk or severity of adverse effects can be increased when Clofarabine is combined with Melphalan.
Prednisone The risk or severity of adverse effects can be increased when Prednisone is combined with Melphalan.
Pemetrexed The risk or severity of adverse effects can be increased when Pemetrexed is combined with Melphalan.
Fludrocortisone The risk or severity of adverse effects can be increased when Fludrocortisone is combined with Melphalan.
Mycophenolate mofetil The risk or severity of adverse effects can be increased when Mycophenolate mofetil is combined with Melphalan.
Daunorubicin The risk or severity of adverse effects can be increased when Daunorubicin is combined with Melphalan.
Irinotecan The risk or severity of adverse effects can be increased when Irinotecan is combined with Melphalan.
Methimazole The risk or severity of adverse effects can be increased when Methimazole is combined with Melphalan.
Etoposide The risk or severity of adverse effects can be increased when Etoposide is combined with Melphalan.
Sulfasalazine The risk or severity of adverse effects can be increased when Sulfasalazine is combined with Melphalan.
Dacarbazine The risk or severity of adverse effects can be increased when Dacarbazine is combined with Melphalan.
Temozolomide The risk or severity of adverse effects can be increased when Temozolomide is combined with Melphalan.
Penicillamine The risk or severity of adverse effects can be increased when Penicillamine is combined with Melphalan.
Prednisolone The risk or severity of adverse effects can be increased when Prednisolone is combined with Melphalan.
Sirolimus The risk or severity of adverse effects can be increased when Sirolimus is combined with Melphalan.
Mechlorethamine The risk or severity of adverse effects can be increased when Mechlorethamine is combined with Melphalan.
Azacitidine The risk or severity of adverse effects can be increased when Azacitidine is combined with Melphalan.
Carboplatin The risk or severity of adverse effects can be increased when Carboplatin is combined with Melphalan.
Methylprednisolone The risk or severity of adverse effects can be increased when Methylprednisolone is combined with Melphalan.
Dactinomycin The risk or severity of adverse effects can be increased when Dactinomycin is combined with Melphalan.
Cytarabine The risk or severity of adverse effects can be increased when Cytarabine is combined with Melphalan.
Azathioprine The risk or severity of adverse effects can be increased when Azathioprine is combined with Melphalan.
Doxorubicin The risk or severity of adverse effects can be increased when Doxorubicin is combined with Melphalan.
Hydroxyurea The risk or severity of adverse effects can be increased when Hydroxyurea is combined with Melphalan.
Busulfan The risk or severity of adverse effects can be increased when Busulfan is combined with Melphalan.
Mycophenolic acid The risk or severity of adverse effects can be increased when Mycophenolic acid is combined with Melphalan.
Topotecan The risk or severity of adverse effects can be increased when Topotecan is combined with Melphalan.
Mercaptopurine The risk or severity of adverse effects can be increased when Mercaptopurine is combined with Melphalan.
Thalidomide The risk or severity of adverse effects can be increased when Thalidomide is combined with Melphalan.
Fludarabine The risk or severity of adverse effects can be increased when Melphalan is combined with Fludarabine.

Target Protein

DNA

Referensi & Sumber

Artikel (PubMed)
  • PMID: 18324787
    Loeber R, Michaelson E, Fang Q, Campbell C, Pegg AE, Tretyakova N: Cross-linking of the DNA repair protein Omicron6-alkylguanine DNA alkyltransferase to DNA in the presence of antitumor nitrogen mustards. Chem Res Toxicol. 2008 Apr;21(4):787-95. doi: 10.1021/tx7004508. Epub 2008 Feb 14.
  • PMID: 7527485
    Povirk LF, Shuker DE: DNA damage and mutagenesis induced by nitrogen mustards. Mutat Res. 1994 Dec;318(3):205-26. doi: 10.1016/0165-1110(94)90015-9.
  • PMID: 8781575
    Lawley PD, Phillips DH: DNA adducts from chemotherapeutic agents. Mutat Res. 1996 Aug 17;355(1-2):13-40. doi: 10.1016/0027-5107(96)00020-6.
  • PMID: 22922522
    Bayraktar UD, Bashir Q, Qazilbash M, Champlin RE, Ciurea SO: Fifty years of melphalan use in hematopoietic stem cell transplantation. Biol Blood Marrow Transplant. 2013 Mar;19(3):344-56. doi: 10.1016/j.bbmt.2012.08.011. Epub 2012 Aug 24.
  • PMID: 27910767
    Kuczma M, Ding ZC, Zhou G: Immunostimulatory Effects of Melphalan and Usefulness in Adoptive Cell Therapy with Antitumor CD4+ T Cells. Crit Rev Immunol. 2016;36(2):179-191. doi: 10.1615/CritRevImmunol.2016017507.
  • PMID: 33922721
    Poczta A, Rogalska A, Marczak A: Treatment of Multiple Myeloma and the Role of Melphalan in the Era of Modern Therapies-Current Research and Clinical Approaches. J Clin Med. 2021 Apr 23;10(9):1841. doi: 10.3390/jcm10091841.

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