Chia Tai-Tianqing (CTTQ) has initiated a clinical study (NCT06218771) of TQB3454, an IDH1 inhibitor, in patients with AML/MDS. This trial started in July 2023, while the study of IDH2 inhibitor TQB3455 was terminated in 2021 due to slow enrollment.
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The first Investigational New Drug (IND) application for TQB3454 was filed for the treatment of solid tumors and blood cancers in China in 2020. The first-in-human clinical trial was initiated in August of that year enrolling patients with advanced solid tumors or hematologic malignancies. While no results from this initial trial have been publicly reported, several other clinical trials for TQB3454 are currently ongoing and recruiting participants.
In 2023, CTTQ initiated a phase 1 clinical study (NCT05987358) of TQB3454 in patients with advanced biliary carcinoma, with an estimated enrollment of 165 participants. IDH1 mutations occur in approximately 13% of patients with intrahepatic cholangiocarcinoma. A phase 3 trial reported that the median progression-free survival (PFS) was extended from 1.4 months to 2.7 months for patients with IDH1m cholangiocarcinoma treated with Ivosidenib compared with placebo. Ivosidenib was approved for the treatment of patients with advanced or metastatic cholangiocarcinoma with an isocitrate dehydrogenase-1 (IDH1) mutation by the US FDA in 2021.
The targeting indication for TQB3454 has shifted back to its original approval of IDH1-mutant Acute Myeloid Leukemia (AML). Now for blood cancer, CTTQ also added the approved MDS indication.
In 2017, CTTQ filed a patent claiming the IDH1 inhibitors with the below formula in the examples.
| Structures |
The compound was tested for its inhibitory activities (IC 50)against IDH1 mutants (R132H and R132C), demonstrating IC50 values less than 20 nM.
| IC50 and PK data |
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