A phase 1 dose-escalation study of checkpoint kinase 1 (CHK1) inhibitor prexasertib in combination with p38 mitogen-activated protein kinase (p38 MAPK) inhibitor ralimetinib in patients with advanced or metastatic cancer.
Adult
Aged
Antineoplastic Agents
/ administration & dosage
Antineoplastic Combined Chemotherapy Protocols
/ administration & dosage
Checkpoint Kinase 1
/ antagonists & inhibitors
Female
Humans
Imidazoles
/ administration & dosage
Male
Middle Aged
Models, Biological
Neoplasms
/ drug therapy
Protein Kinase Inhibitors
/ administration & dosage
Pyrazines
/ administration & dosage
Pyrazoles
/ administration & dosage
Pyridines
/ administration & dosage
Treatment Outcome
p38 Mitogen-Activated Protein Kinases
/ antagonists & inhibitors
CHK1
LY2606368
Prexasertib
Ralimetinib
p38 MAPK
Journal
Investigational new drugs
ISSN: 1573-0646
Titre abrégé: Invest New Drugs
Pays: United States
ID NLM: 8309330
Informations de publication
Date de publication:
08 2020
08 2020
Historique:
received:
09
08
2019
accepted:
22
10
2019
pubmed:
11
11
2019
medline:
10
9
2021
entrez:
11
11
2019
Statut:
ppublish
Résumé
Purpose The primary objective was to determine the recommended Phase 2 dose (RP2D) of checkpoint kinase 1 inhibitor, prexasertib, in combination with the p38 mitogen-activated protein kinase inhibitor, ralimetinib, which may be safely administered to patients with advanced cancer. Methods This Phase 1, nonrandomized, open-label, dose-escalation study of prexasertib+ralimetinib included patients with advanced and/or metastatic cancer, followed by a planned cohort expansion in patients with colorectal or non-small-cell lung cancer with KRAS and/or BRAF mutations. Intravenous prexasertib was administered at 60 mg/m
Identifiants
pubmed: 31707688
doi: 10.1007/s10637-019-00873-6
pii: 10.1007/s10637-019-00873-6
doi:
Substances chimiques
Antineoplastic Agents
0
Imidazoles
0
Protein Kinase Inhibitors
0
Pyrazines
0
Pyrazoles
0
Pyridines
0
prexasertib
0
ralimetinib
73I34XW4HD
Checkpoint Kinase 1
EC 2.7.11.1
p38 Mitogen-Activated Protein Kinases
EC 2.7.11.24
Types de publication
Clinical Trial, Phase I
Journal Article
Multicenter Study
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM