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DRUG:

unecritinib (TQ-B3101)

i
Other names: TQ-B3101, TQ B3101
Company:
Sino Biopharm
Drug class:
ALK inhibitor, ROS1 inhibitor, c-MET inhibitor
Related drugs:
over1year
Efficacy, safety and pharmacokinetics of Unecritinib (TQ-B3101) for patients with ROS1 positive advanced non-small cell lung cancer: a Phase I/II Trial. (PubMed, Signal Transduct Target Ther)
This phase I/II trial characterized the tolerability, safety, and antitumor activities of unecritinib, a novel derivative of crizotinib and a multi-tyrosine kinase inhibitor targeting ROS1, ALK, and c-MET, in advanced tumors and ROS1 inhibitor-naive advanced or metastatic non-small cell lung cancer (NSCLC) harboring ROS1 rearrangements. Treatment-related ocular disorders and neurotoxicity occurred in 28.1% and 34.4% of patients, respectively, but none was grade 3 or higher. Unecritinib is efficacious and safe for ROS1 inhibitor-naive patients with ROS1-positive advanced NSCLC, particularly patients with brain metastases at baseline, strongly supporting that unecritinib should become one of the standards of care for ROS1-positive NSCLC.ClinicalTrials.gov identifier: NCT03019276 and NCT03972189.
P1/2 data • PK/PD data • Clinical Trial,Phase II • Journal • Metastases
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ALK (Anaplastic lymphoma kinase) • MET (MET proto-oncogene, receptor tyrosine kinase) • ROS1 (Proto-Oncogene Tyrosine-Protein Kinase ROS)
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ROS1 positive • ROS1 rearrangement
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Xalkori (crizotinib) • unecritinib (TQ-B3101)
2years
Phase I Study of Tq-B3101 in Pediatric Patients with Relapsed/Refractory Anaplastic Lymphoma Kinase Positive Anaplastic Large Cell Lymphoma (ASH 2022)
The results of ADVL0912 (NCT00939770) and A8081013 (NCT01121588) studies suggest that the ALK inhibitor crizotinib has good efficacy and safety in the treatment of ALK+ALCL. Responses were durable and ongoing, and treatment was well tolerated. Further investigation is warranted to find the MTD and confirm the efficacy of TQ-B3101.
Clinical • P1 data
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ALK (Anaplastic lymphoma kinase) • MET (MET proto-oncogene, receptor tyrosine kinase) • ROS1 (Proto-Oncogene Tyrosine-Protein Kinase ROS)
|
ALK positive
|
Xalkori (crizotinib) • unecritinib (TQ-B3101)
almost3years
The efficacy and safety of TQ-B3101 monotherapy in the first line treatment in patients with ROS1 positive non-small cell lung cancer (ELCC 2022)
Most common TRAEs were AST increased (73.9%), ALT increased (72.1%), emesis (63.1%), neutrophils count decrease (56.8%), leukocyte count decrease (52.3%), sinus bradycardia (52.3%), and diarrhea (43.2%). Conclusions For the first-line treatment of ROS1-positive locally advanced or metastatic NSCLC patients, TQ-B3101 showed the promising efficacy with a manageable safety profile, offering a new first-line therapeutic strategy.
Clinical
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ALK (Anaplastic lymphoma kinase) • ROS1 (Proto-Oncogene Tyrosine-Protein Kinase ROS)
|
ROS1 positive
|
unecritinib (TQ-B3101)
almost3years
Population Pharmacokinetic Modeling and Simulation of TQ-B3101 to Inform Dosing in Pediatric Patients With Solid Tumors. (PubMed, Front Pharmacol)
The projected exposure of TQ-B3101M in virtual pediatric population following the body surface area tiered dosing regimen was similar to that in children pediatric patients after the recommended pediatric dose of crizotinib (280 mg/m2 twice daily), an analog of TQ-B3101M. A population pharmacokinetic model was developed to provide optimal dose of regimen for further development of TQ-B3101 in pediatric patients with anaplastic large cell lymphoma.
PK/PD data • Journal
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ALK (Anaplastic lymphoma kinase)
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ALK positive
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Xalkori (crizotinib) • unecritinib (TQ-B3101)
over4years
[VIRTUAL] A phase I study to evaluate safety, tolerability, pharmacokinetics, and preliminary antitumor activity of TQ-B3101. (ASCO 2020)
Preclinical studies showed TQ-B3101 had a better Inhibition activity and duration compared with equimolar crizotinib. TQ-B3101 was well tolerated and showed preliminary antitumor activity in ALK+, ROS1+ and MET amplification pts. Recommended phase II dose (RP2D) might be 300mg BID according longtime safety data. Further anti-tumor research in pts with ROS1+ is under going as multicenter clinical study in China.
Clinical • P1 data • PK/PD data
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ROS1 (Proto-Oncogene Tyrosine-Protein Kinase ROS)
|
MET amplification
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Xalkori (crizotinib) • unecritinib (TQ-B3101)