Primary objectives: To evaluate the safety and tolerability of single/multiple administrations in patients with advanced solid tumors, determine the maximum tolerated dose and recommended dose for Phase II trials, and evaluate the effect of food on the pharmacokinetics of patients after a single dose. Secondary objectives: 1) To analyze the pharmacokinetic properties of single/multiple administrations; 2) To preliminarily evaluate the anti-tumor activity; 3) To evaluate the effect of food on the safety and tolerability of a single dose.

Start Date23 Apr 2020

Sponsor / Collaborator

Tianjin Chase Sun Pharmaceutical Co., Ltd.

[+1]

100 Clinical Results associated with IMMH-010

100 Translational Medicine associated with IMMH-010

100 Patents (Medical) associated with IMMH-010

Literatures (Medical) associated with IMMH-010

PharmaceuticsQ3 · MEDICINE

Metabolism and Interspecies Variation of IMMH-010, a Programmed Cell Death Ligand 1 Inhibitor Prodrug

Q3 · MEDICINE

ArticleOA

Author: Liu, Xiao ; Dong, Kai ; Luo, Lijun ; Wang, Shuting ; Zou, Xiaowen ; Li, Yan ; Liu, Yuke ; Yao, Xiaoqing ; Wang, Yuchen ; Chen, Xiaoguang ; Sheng, Li

IMMH-010 is an ester prodrug of YPD-29B, a potent programmed cell death ligand 1 (PD-L1) inhibitor. The metabolism of IMMH-010 was investigated and compared in various species. Four metabolites of IMMH-010 were identified, and the major metabolite was the parent compound, YPD-29B, which was mainly catalyzed by carboxylesterase 1 (CES1). We observed IMMH-010 metabolism in the plasma of various species. IMMH-010 was rapidly metabolized to YPD-29B in rat and mouse plasma, whereas it remained stable in human and monkey plasma. In the liver S9 fractions of human, monkey, dog, and rat, IMMH-010 was quickly transformed to YPD-29B with no obvious differences among species. In addition, the transformation ratio of IMMH-010 to YPD-29B was low in rat and human intestines, which indicated that the intestine was not an important site for IMMH-010 hydrolysis. Moreover, we demonstrated the remarkable antitumor efficacy of IMMH-010 in B16F10 melanoma and MC38 colon carcinoma xenograft mouse models. We also compared the pharmacokinetic profiles of IMMH-010 in rodents and primates. After oral administration of IMMH-010, the general exposure of active metabolite YPD-29B was slightly lower in primates than in rodents, suggesting that data should be extrapolated cautiously from rodents to humans.

Frontiers in PharmacologyQ2 · MEDICINE

Simultaneous Determination of a Novel PD-L1 Inhibitor, IMMH-010, and Its Active Metabolite, YPD-29B, in Rat Biological Matrices by Polarity-Switching Liquid Chromatography-Tandem Mass Spectrometry: Application to ADME Studies

Q2 · MEDICINE

ArticleOA

Author: Yao, Xiaoqing ; Zou, Xiaowen ; Liu, Yuke ; Jiang, Jianwei ; Dong, Kai ; Liu, Xiao ; Sheng, Li ; Li, Yan ; Chen, Xiaoguang ; Feng, Zhiqiang

IMMH-010 is a prodrug of YPD-29B, which is a novel PD-L1 inhibitor. A specific and sensitive LC-MS/MS method with polarity switching was developed and validated for the simultaneous determination of IMMH-010 and YPD-29B in rat plasma, liver, brain, urine and fecal samples. Method validation was investigated to demonstrate the lower limit of quantification linearity, precision and accuracy, matrix effect and recovery, stability and dilution reliability for IMMH-010 and YPD-29B. This validated method was successfully applied to investigate the pharmacokinetics, tissue distribution, and excretion of IMMH-010 and YPD-29B in rats. After oral administration of IMMH-010 maleate to rats, IMMH-010 was rapidly and extensively converted to the active metabolite YPD-29B. The areas under the plasma concentration-time curve (AUC) of IMMH-010 and YPD-29B were proportional to the dose in the range of 10–100 mg/kg. IMMH-010 was primarily distributed in the adrenal gland, lymph nodes, heart, liver and spleen. YPD-29B was mainly observed in the liver, lymph, kidney, and lung. Approximately 28.81% of the IMMH-010 dose was recovered in the urine and feces within 72 h, including unchanged IMMH-010 (7.99%) and YPD-29B (20.82%). The results of this study may be useful as a reference for further development of IMMH-010 and PD-L1 inhibitors.Clinical Trial Registration: [https://clinicaltrials.gov/ct2/show/NCT04343859?term=IMMH-010&draw=2&rank=1], identifier [NCT04343859]."

100 Deals associated with IMMH-010

R&D Status

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Indication	Highest Phase	Country/Location	Organization	Date
Brain Cancer	Phase 2	-	Tianjin Chase Sun Pharmaceutical Co., Ltd.	-
Advanced Malignant Solid Neoplasm	Phase 1	CN	Institute of Materia Medica	23 Apr 2020
Advanced Malignant Solid Neoplasm	Phase 1	CN	Tianjin Chase Sun Pharmaceutical Co., Ltd.	23 Apr 2020

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