P1, N=78, Completed, Ono Pharmaceutical Co. Ltd | Active, not recruiting --> Completed | Trial completion date: Apr 2026 --> Jun 2025 | Trial primary completion date: Apr 2026 --> Jun 2025

Guided by a scaffold-hopping strategy based on G-749 (denfivontinib), a series of quinazoline-based derivatives was designed and synthesized to explore structure-activity relationships (SAR)...Mechanism studies indicated that W4 induced G0/G1 cell cycle arrest and apoptosis, accompanied by a reduction in intracellular reactive oxygen species levels and a loss of mitochondrial membrane potential. Collectively, these results identified W4 as a potent FLT3 inhibitor and provided valuable SAR insights for further scaffold optimization.

P1/2, N=120, Active, not recruiting, Qurient Co., Ltd. | Recruiting --> Active, not recruiting | Trial completion date: Jun 2026 --> Mar 2028 | Trial primary completion date: Oct 2025 --> Dec 2027

Herein, we develop an MRX-2843 (MerTK inhibitor) and Mn2+ codelivered defective metal-organic framework (copper-2,3,6,7,10,11-hexaiminotriphenylene (Cu-HITP))-based single-site nanozyme (Ir@D-Cu-HITP-MMP) for antitumor immunotherapy via innate immune-checkpoint blockade...This synergizes with Mn2+ to enhance the stimulator of interferon genes (STING) activation, triggering robust immune responses. Overall, Ir@D-Cu-HITP-MMP demonstrates potent antitumor effects by activating powerful innate and adaptive immune responses.

P1, N=16, Recruiting, Qurient Co. Ltd.

Combining CTX with the next generation MERTK-selective inhibitor UNC2371 (MRX-2843) drives complete remissions in both models, but durable long-term responses occurred selectively in the basal-like subtype model. Suppressive myeloid programing limits effective adaptive immune engagement in TNBC usually resulting in ICB treatment resistance and tumor recurrence. This study identifies a therapeutically actionable myeloid interferon checkpoint in which MERTK inhibition stabilizes CXCL9⁺ monocyte-macrophage programming to promote CD4⁺ T cell dependent immune memory and durable tumor control in basal-like TNBC.

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

P1, N=50, Recruiting, Meryx, Inc. | Trial completion date: Mar 2026 --> Sep 2026 | Trial primary completion date: Dec 2025 --> Jul 2026

P1, N=18, Recruiting, Qurient Co., Ltd. | Not yet recruiting --> Recruiting

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

Tamnorzatinib alone and in combination with venetoclax was safe and well tolerated but failed to induce robust clinical efficacy in R/R AML.

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.