^
Contact us  to learn more about
our Premium Content:  News alerts, weekly reports and conference planners
DRUG CLASS:

MERTK inhibitor

12d
Pharmacokinetic and Safety Study of MRX-2843 in Adults With Relapsed/Refractory Advanced and/or Metastatic Solid Tumors (clinicaltrials.gov)
P1, N=42, Completed, Meryx, Inc. | Active, not recruiting --> Completed | Trial completion date: Apr 2025 --> Dec 2025 | Trial primary completion date: Feb 2025 --> Dec 2025
Trial completion • Trial completion date • Trial primary completion date • First-in-human
|
MRX2843
12d
Pharmacokinetic and Safety Study of MRX-2843 in Adolescents and Adults With Relapsed/Refractory AML, ALL, or MPAL (clinicaltrials.gov)
P1, N=50, Recruiting, Meryx, Inc. | Trial completion date: Mar 2026 --> Sep 2026 | Trial primary completion date: Dec 2025 --> Jul 2026
Trial completion date • Trial primary completion date
|
MRX2843
21d
A Study to Evaluate Adrixetinib (Q702) in Adults With Active Chronic Graft-Versus-Host Disease (clinicaltrials.gov)
P1, N=18, Recruiting, Qurient Co., Ltd. | Not yet recruiting --> Recruiting
Enrollment open
|
adrixetinib (Q702)
21d
Oral Axl/Mer/CSF1R Selective Tyrosine Kinase Inhibitor in Patients With Advanced Solid Tumor (clinicaltrials.gov)
P1, N=51, Completed, Qurient Co., Ltd. | Active, not recruiting --> Completed | N=78 --> 51 | Trial completion date: Feb 2025 --> Dec 2025 | Trial primary completion date: Dec 2024 --> Dec 2025
Trial completion • Enrollment change • Trial completion date • Trial primary completion date
|
adrixetinib (Q702)
1m
P1 data • P2 data • Journal
|
AXL (AXL Receptor Tyrosine Kinase) • MERTK (MER Proto-Oncogene, Tyrosine Kinase)
|
Venclexta (venetoclax) • tamnorzatinib (ONO-7475)
3ms
Targeting MERTK tyrosine kinase: Virtual screening and molecular dynamics insights for anti-cancer drug development. (PubMed, PLoS One)
We used known compound UNC2025 as positive control and one million compounds was retrieved from different databases (OTAVA, ZINC, ChEMBL) and docked with MERTK protein...The study finds critical residues which serve a vital part in binding with the inhibitor and the active site of the MERTK protein, i.e., Phe598, Gly599, Lys619, Arg629, Glu633, Glu637, Arg722, Asp723, Arg727, Asp741, Gly743, Leu744, Lys746, Arg758, Ala760, and Lys761 through decomposed binding free energy analysis. This study focuses on the pursuit of several MERTK protein targets, which could have consequences for the development of novel therapeutics for various cancers.
Journal
|
MERTK (MER Proto-Oncogene, Tyrosine Kinase) • LRIG1 (Leucine Rich Repeats And Immunoglobulin Like Domains 1) • LIG3 (DNA Ligase 3)
|
UNC2025
3ms
A Study Exploring the Safety and Tolerability of INCB081776 in Participants With Advanced Malignancies (clinicaltrials.gov)
P1, N=83, Terminated, Incyte Corporation | Active, not recruiting --> Terminated; The study was terminated after careful review of the overall clinical activity of this compound and a lack of robust efficacy. The study closure is not based on safety concerns.
Trial termination
|
FLT3 (Fms-related tyrosine kinase 3) • MSI (Microsatellite instability) • IDH1 (Isocitrate dehydrogenase (NADP(+)) 1) • IDH2 (Isocitrate Dehydrogenase (NADP(+)) 2)
|
MSI-H/dMMR • FLT3-ITD mutation • IDH wild-type
|
Zynyz (retifanlimab-dlwr) • INCB81776
5ms
New P1 trial
|
adrixetinib (Q702)
6ms
NAT10 Increases Lysosomal Acidification to Promote Esophageal Cancer Metastasis via ac4C Acetylation of ATP6V0E1 mRNA. (PubMed, Adv Sci (Weinh))
Furthermore, G-749 is screened and identified as a novel NAT10 inhibitor capable of effectively impeding lysosomal acidification and tumor metastasis by disrupting the NAT10-Ubiquitin-specific Peptidase 39 (USP39) interaction. Overall, the results unveil a novel role of ac4C modifications in regulating lysosomal acidification and propose a potential strategy by targeting NAT10 to inhibit esophageal cancer metastasis.
Journal
|
CDH1 (Cadherin 1)
|
denfivontinib (SKI-G-801)
7ms
Study of ONO-7475 in Combination With Osimertinib in EGFR Gene Mutation-positive Non-small Cell Lung Cancer (clinicaltrials.gov)
P1, N=78, Active, not recruiting, Ono Pharmaceutical Co. Ltd | Trial completion date: Oct 2025 --> Apr 2026 | Trial primary completion date: Oct 2025 --> Apr 2026
Trial completion date • Trial primary completion date
|
Tagrisso (osimertinib) • tamnorzatinib (ONO-7475)
8ms
Glycopolymeric Nanoparticles Block Breast Cancer Growth by Inhibiting Efferocytosis in the Tumor Microenvironment. (PubMed, ACS Appl Nano Mater)
Lastly, UNC2025-PMAM NPs significantly reduced tumor volume compared to free UNC2025, showing greater therapeutic efficacy in a model of triple-negative breast cancer. These glycopolymer-based, efferocytosis-blocking NPs have promise both as a class of standalone cancer immunotherapy and as an adjuvant to improve response rates to checkpoint immunotherapy.
Journal
|
MERTK (MER Proto-Oncogene, Tyrosine Kinase) • MRC1 (Mannose Receptor C-Type 1)
|
UNC2025
8ms
Targeting the ZMYM2-ANXA9 Axis with FLT3 Inhibitor G749 Overcomes Oxaliplatin Resistance in Colorectal Cancer. (PubMed, Biomedicines)
The ZMYM2-ANXA9 signaling axis drives chemoresistance and tumor progression in CRC. FLT3 inhibition by G749 effectively downregulates ANXA9 and sensitizes tumors to chemotherapy, highlighting a novel therapeutic approach for chemoresistant CRC.
Journal
|
FLT3 (Fms-related tyrosine kinase 3) • ZMYM2 (Zinc Finger MYM-Type Containing 2)
|
oxaliplatin • denfivontinib (SKI-G-801)