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 …

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 …

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 …

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 …

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 …

2021 FDA TIDES (peptides and oligonucleotides) harvest

D Al Shaer, O Al Musaimi, F Albericio, BG de la Torre - Pharmaceuticals, 2022 - mdpi.com
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 …

[HTML][HTML] The approval and withdrawal of melphalan flufenamide (melflufen): Implications for the state of the FDA.

T Olivier, V Prasad - Translational Oncology, 2022 - Elsevier
In October 2021, melphalan flufenamide (melflufen) was withdrawn from the US market for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 …

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 …

Melflufen: a peptide–drug conjugate for the treatment of multiple myeloma

MV Mateos, J Bladé, S Bringhen, EM Ocio… - Journal of clinical …, 2020 - mdpi.com
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 …

Aminopeptidase expression in multiple myeloma associates with disease progression and sensitivity to melflufen

JJ Miettinen, R Kumari, GA Traustadottir… - Cancers, 2021 - mdpi.com
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 …