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Melflufen :
Melflufen : A Peptide-Drug Conjugate for the Treatment of Multiple Myeloma
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- Mateos, Maria-Victoria (author)
- Hosp Clin Univ Salamanca IBSAL CIC, Salamanca 37007, Spain.
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- Blade, Joan (author)
- Hosp Clin Barcelona, Inst Invest Biomed August Pi I Sunyer, Hematol Dept, Barcelona 08036, Spain.
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- Bringhen, Sara (author)
- Univ Torino, Azienda Osped Univ Citta Salute & Sci Torino, Div Hematol, Myeloma Unit, I-10126 Turin, Italy.
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- Ocio, Enrique M. (author)
- Univ Cantabria, Univ Hosp Marques Valdecilla IDIVAL, Santander 39008, Spain.
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- Efebera, Yvonne (author)
- Ohio State Univ, Dept Internal Med, Div Hematol, Comprehens Canc Ctr, Columbus, OH 43210 USA.
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- Pour, Ludek (author)
- Univ Hosp Brno, Dept Internal Med Hematol & Oncol, Brno 62500, Czech Republic.
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- Gay, Francesca (author)
- Univ Torino, Azienda Osped Univ Citta Salute & Sci Torino, Div Hematol, Myeloma Unit, I-10126 Turin, Italy.
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- Sonneveld, Pieter (author)
- Erasmus MC Canc Inst, NL-3075 EA Rotterdam, Netherlands.
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- Gullbo, Joachim (author)
- Uppsala universitet,Institutionen för medicinska vetenskaper
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- Richardson, Paul G. (author)
- Harvard Med Sch, Jerome Lipper Multiple Myeloma Ctr, Dana Farber Canc Inst, Boston, MA 02215 USA.
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Hosp Clin Univ Salamanca IBSAL CIC, Salamanca 37007, Spain Hosp Clin Barcelona, Inst Invest Biomed August Pi I Sunyer, Hematol Dept, Barcelona 08036, Spain. (creator_code:org_t)
- 2020-09-27
- 2020
- English.
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In: Journal of Clinical Medicine. - : MDPI AG. - 2077-0383. ; 9:10
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Abstract
Subject headings
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- Despite the availability of new therapies that have led to improved outcomes for patients with multiple myeloma, most patients will eventually relapse. With triplet and even quadruplet combination therapies becoming standard in the first and second line, many patients will have few treatment options after second-line treatment. Melflufen (melphalan flufenamide) is a first-in-class peptide-drug conjugate (PDC) that targets aminopeptidases and rapidly releases alkylating agents into tumor cells. Once inside the tumor cells, melflufen is hydrolyzed by peptidases to release alkylator molecules, which become entrapped. Melflufen showed anti-myeloma activity in myeloma cells that were resistant to bortezomib and the alkylator melphalan. In early phase studies (O-12-M1 and HORIZON [OP-106]), melflufen plus dexamethasone has demonstrated encouraging clinical activity and a manageable safety profile in heavily pretreated patients with relapsed/refractory multiple myeloma, including those with triple-class refractory disease and extramedullary disease. The Phase III OCEAN study (OP-104) is further evaluating melflufen plus dexamethasone in patients with relapsed/refractory multiple myeloma. The safety profile of melflufen is characterized primarily by clinically manageable hematologic adverse events. Melflufen, with its novel mechanism of action, has the potential to provide clinically meaningful benefits to patients with relapsed/refractory multiple myeloma, including those with high unmet needs.
Subject headings
- MEDICIN OCH HÄLSOVETENSKAP -- Klinisk medicin -- Cancer och onkologi (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Clinical Medicine -- Cancer and Oncology (hsv//eng)
- MEDICIN OCH HÄLSOVETENSKAP -- Medicinska och farmaceutiska grundvetenskaper -- Cell- och molekylärbiologi (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Basic Medicine -- Cell and Molecular Biology (hsv//eng)
Keyword
- melflufen
- melphalan flufenamide
- peptide–
- drug conjugate
- multiple myeloma
- new drugs
- drug combinations
Publication and Content Type
- ref (subject category)
- for (subject category)
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- By the author/editor
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Mateos, Maria-Vi ...
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Blade, Joan
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Bringhen, Sara
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Ocio, Enrique M.
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Efebera, Yvonne
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Pour, Ludek
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Gay, Francesca
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Sonneveld, Piete ...
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Gullbo, Joachim
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Richardson, Paul ...
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- MEDICAL AND HEALTH SCIENCES
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MEDICAL AND HEAL ...
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and Clinical Medicin ...
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and Cancer and Oncol ...
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- MEDICAL AND HEALTH SCIENCES
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MEDICAL AND HEAL ...
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and Basic Medicine
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and Cell and Molecul ...
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Uppsala University