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@article{1775027,
author = {Mateos, MV and Blade, J and Bringhen, S and Ocio, EM and Efebera, Y and Pour, Luděk and Gay, F and Sonneveld, P and Gullbo, J and Richardson, PG},
article_location = {BASEL},
article_number = {10},
doi = {http://dx.doi.org/10.3390/jcm9103120},
keywords = {melflufen; melphalan flufenamide; peptide– drug conjugate; multiple myeloma; new drugs; drug combinations},
language = {eng},
issn = {2077-0383},
journal = {Journal of Clinical Medicine},
note = {Bez afiliace k MU.},
title = {Melflufen: A Peptide-Drug Conjugate for the Treatment of Multiple Myeloma},
volume = {9},
year = {2020}
}
TY - JOUR
ID - 1775027
AU - Mateos, MV - Blade, J - Bringhen, S - Ocio, EM - Efebera, Y - Pour, Luděk - Gay, F - Sonneveld, P - Gullbo, J - Richardson, PG
PY - 2020
TI - Melflufen: A Peptide-Drug Conjugate for the Treatment of Multiple Myeloma
JF - Journal of Clinical Medicine
VL - 9
IS - 10
PB - MDPI
SN - 20770383
N1 - Bez afiliace k MU.
KW - melflufen
KW - melphalan flufenamide
KW - peptide– drug conjugate
KW - multiple myeloma
KW - new drugs
KW - drug combinations
N2 - 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.
ER -
MATEOS, MV, J BLADE, S BRINGHEN, EM OCIO, Y EFEBERA, Luděk POUR, F GAY, P SONNEVELD, J GULLBO and PG RICHARDSON. Melflufen: A Peptide-Drug Conjugate for the Treatment of Multiple Myeloma. \textit{Journal of Clinical Medicine}. BASEL: MDPI, 2020, vol.~9, No~10, 16 pp. ISSN~2077-0383. Available from: https://dx.doi.org/10.3390/jcm9103120.
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