Progress and future directions with peptide-drug conjugates for targeted cancer therapy
J Lindberg, J Nilvebrant, PÅ Nygren, F Lehmann - Molecules, 2021 - mdpi.com
We review drug conjugates combining a tumor-selective moiety with a cytotoxic agent as
cancer treatments. Currently, antibody-drug conjugates (ADCs) are the most common drug …
cancer treatments. Currently, antibody-drug conjugates (ADCs) are the most common drug …
The mercapturic acid pathway
PE Hanna, MW Anders - Critical reviews in toxicology, 2019 - Taylor & Francis
The mercapturic acid pathway is a major route for the biotransformation of xenobiotic and
endobiotic electrophilic compounds and their metabolites. Mercapturic acids (N-acetyl-l …
endobiotic electrophilic compounds and their metabolites. Mercapturic acids (N-acetyl-l …
Melflufen and dexamethasone in heavily pretreated relapsed and refractory multiple myeloma
PG Richardson, A Oriol, A Larocca, J Bladé… - Journal of Clinical …, 2021 - ascopubs.org
PURPOSE Melphalan flufenamide (melflufen) is a first-in-class peptide-drug conjugate that
targets aminopeptidases and rapidly and selectively releases alkylating agents into tumor …
targets aminopeptidases and rapidly and selectively releases alkylating agents into tumor …
Melflufen or pomalidomide plus dexamethasone for patients with multiple myeloma refractory to lenalidomide (OCEAN): a randomised, head-to-head, open-label …
FH Schjesvold, MA Dimopoulos, S Delimpasi… - The Lancet …, 2022 - thelancet.com
Background Melphalan flufenamide (melflufen), an alkylating peptide-drug conjugate, plus
dexamethasone showed clinical activity and manageable safety in the phase 2 HORIZON …
dexamethasone showed clinical activity and manageable safety in the phase 2 HORIZON …
Melflufen plus dexamethasone in relapsed and refractory multiple myeloma (O-12-M1): A multicentre, international, open-label, phase 1–2 study
PG Richardson, S Bringhen, P Voorhees… - The Lancet …, 2020 - thelancet.com
Background Multiple myeloma is an incurable haematological malignancy, representing
over 10% of haematological cancers in the USA. We did a phase 1–2 study of melflufen and …
over 10% of haematological cancers in the USA. We did a phase 1–2 study of melflufen and …
2021 FDA TIDES (peptides and oligonucleotides) harvest
From the medical, pharmaceutical, and social perspectives, 2021 has been a year
dominated by the COVID-19 pandemic. However, despite this global health crisis, the …
dominated by the COVID-19 pandemic. However, despite this global health crisis, the …
[HTML][HTML] The approval and withdrawal of melphalan flufenamide (melflufen): Implications for the state of the FDA.
In October 2021, melphalan flufenamide (melflufen) was withdrawn from the US market for
the treatment of multiple myeloma. The decision occurred based on results from a phase 3 …
the treatment of multiple myeloma. The decision occurred based on results from a phase 3 …
Evolution of nitrogen-based alkylating anticancer agents
F Lehmann, J Wennerberg - Processes, 2021 - mdpi.com
Despite the significant progress in anticancer drug development over recent years, there is a
vital need for newer agents with unique, but still effective, mechanisms of action in order to …
vital need for newer agents with unique, but still effective, mechanisms of action in order to …
Melflufen: a peptide–drug conjugate for the treatment of multiple myeloma
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 …
multiple myeloma, most patients will eventually relapse. With triplet and even quadruplet …
Aminopeptidase expression in multiple myeloma associates with disease progression and sensitivity to melflufen
Simple Summary The aims of this study were to investigate aminopeptidase expression in
multiple myeloma and to identify the aminopeptidases responsible for the activation of the …
multiple myeloma and to identify the aminopeptidases responsible for the activation of the …