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Last update 21 Mar 2025
Envonalkib
Last update 21 Mar 2025
Overview
Basic Info
Drug Type Small molecule drug |
Synonyms 依奉阿克, CT-1139, TQ B3139 + [1] |
Target |
Action inhibitors |
Mechanism ALK inhibitors(Anaplastic lymphoma kinase inhibitors), ROS1 inhibitors(Proto-oncogene tyrosine-protein kinase ROS inhibitors), c-Met inhibitors(Hepatocyte growth factor receptor inhibitors) |
Therapeutic Areas |
Active Indication |
Originator Organization |
Active Organization |
Inactive Organization- |
Drug Highest PhaseApproved |
First Approval Date China (11 Jun 2024), |
RegulationSpecial Review Project (China) |
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Structure/Sequence
Molecular FormulaC24H26Cl2FN5O2 |
InChIKeyBVGDAZBTIVRTGO-UONOGXRCSA-N |
CAS Registry1621519-26-3 |
Related
11
Clinical Trials associated with EnvonalkibCTR20220526
[14C]TQ-B3139在中国成年男性健康受试者体内的吸收、代谢和排泄临床试验-[14C] TQ-B3139人体物质平衡及生物转化研究
[Translation] [14C]TQ-B3139 Absorption, Metabolism and Excretion Clinical Trial in Chinese Adult Male Healthy Subjects - [14C]TQ-B3139 Human Material Balance and Biotransformation Study
NCT04675060
A Study of the Effect of High-fat Meal on the Pharmacokinetics of Oral TQ-B3139 Capsules in Patients With Solid Tumor
CTR20202043
高脂饮食对肿瘤患者口服TQ-B3139胶囊药代动力学的影响研究
[Translation] Effect of high-fat diet on the pharmacokinetics of oral TQ-B3139 capsules in cancer patients
100 Clinical Results associated with Envonalkib
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100 Translational Medicine associated with Envonalkib
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100 Patents (Medical) associated with Envonalkib
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7
Literatures (Medical) associated with Envonalkib01 Nov 2024Cancer chemotherapy and pharmacology
Pharmacokinetics, mass balance, and metabolism of [14C]envonalkib (TQ-B3139), a novel ALK tyrosine kinase inhibitor, in healthy Chinese subjects
Article
Author: Wang, Xunqiang ; Wan, Xiaojing ; Yan, Shu ; Wang, Xin ; Zhang, Hua ; Yu, Ding ; Diao, Xingxing ; Ma, Sheng ; Ding, Dawei ; Miao, Liyan
PURPOSE:
Envonalkib (TQ-B3139) is a novel, potent anaplastic lymphoma kinase (ALK) tyrosine kinase inhibitor used to treat ALK-positive non-small cell lung cancer. This phase I mass balance study investigated the pharmacokinetics, metabolism, and excretion of 14C-radiolabeled envonalkib in healthy Chinese male subjects.
METHODS:
A single oral dose of 600 mg (150 µCi) [14C]envonalkib was administered to healthy male subjects under fasted state. Samples of blood, urine and feces were collected for quantitative determination of total radioactivity and unchanged envonalkib, and the metabolites identification.
RESULTS:
After dosing, the median Tmax of radioactivity was 4 h and the mean t1/2 was 65.2 h in plasma. The exposure of total radioactivity was much higher than that of unchanged envonalkib in plasma. The mean total recovery of the radiolabeled dose was 93.93% over 504 h post-dose, with 15.23% in urine and 78.71% in feces. Envonalkib underwent extensive metabolism and a total of 15 metabolites were identified in plasma, urine, and feces. Unchanged envonalkib and its major metabolite M315 were the main components in plasma, accounting for 20.37% and 33.33% of total plasma radioactivity. In urine, O-dealkylation metabolite M315 was the major component accounted for 7.98% of dose. In feces, 16.01% of dose was excreted as cysteine conjugate M434-1. Envonalkib was well tolerated and there were no serious adverse events observed in the study.
CONCLUSION:
Envonalkib was extensively metabolized prior to excretion and eliminated primarily as metabolites via feces.
01 Aug 2024Translational Lung Cancer Research
Efficacy of ALK inhibitors in Asian patients with ALK inhibitor-naïve advanced ALK-positive non-small cell lung cancer: a systematic review and network meta-analysis
Article
Author: Wang, Chengyan ; Huang, Shanshan ; Li, Xuchang ; Xia, Yangchen ; Chu, Qian
Background:
A previous network meta-analysis (NMA) compared the efficacy of anaplastic lymphoma kinase (ALK) inhibitors in ALK-positive non-small cell lung cancer (NSCLC). The phase III INSPIRE study of iruplinalkib was published recently. The present study aimed to add the results related to iruplinalkib to the NMA.
Methods:
A systematic literature search was performed in PubMed, Embase, Cochrane Library, Google, and Baidu. Randomized controlled trials (RCTs) reporting the independent review committee-assessed progression-free survival (PFS), objective response rate (ORR), or disease control rate (DCR) results of Asian patients with ALK inhibitor-naïve advanced ALK-positive NSCLC were eligible for inclusion in the NMA. Risk of bias was assessed using the Cochrane Risk of Bias 2 tool. Bayesian fixed-effect models were used for the direct and indirect pairwise comparisons. This study was registered with PROSPERO (CRD42024555299).
Results:
Eight studies, involving 1,477 Asian patients and seven treatments (crizotinib, alectinib, brigatinib, ensartinib, envonalkib, iruplinalkib, and lorlatinib), were included in the NMA. In terms of the overall risks of bias, all of the studies had "some concerns". All the next-generation ALK inhibitors were statistically superior to crizotinib in terms of PFS. Iruplinalkib had the best surface under the cumulative ranking curve (74.0%), followed by brigatinib (69.1%) and ensartinib (63.7%). Most of the pairwise comparisons did not reveal significant differences in the ORR and DCR. In terms of both the ORR and DCR, alectinib ranked first, followed by lorlatinib.
Conclusions:
Next-generation ALK inhibitors had better efficacy than crizotinib in the treatment of Asian patients with ALK inhibitor-naïve advanced ALK-positive NSCLC. Iruplinalkib may have more favorable PFS benefit than other ALK inhibitors for Asians.
01 Sep 2022European journal of cancer (Oxford, England : 1990)
First-in-human phase I study of TQ-B3139 (CT-711) in advanced non-small cell lung cancer patients with ALK and ROS1 rearrangements
Article
Author: Zhang, Zhonghan ; Zhang, Yang ; Wan, Xiaojing ; Yang, Haiyan ; Pan, Hui ; Li, Su ; Fang, Wenfeng ; Liu, Jingwen ; Wang, Xunqiang ; Zhang, Yongchang ; Han, Xi ; Xiong, Yi ; Liu, Li ; Yang, Nong ; Zhao, Yuanyuan ; Zhang, Li ; Zhao, Hongyun ; Zhou, Chunhua ; Ma, Yuxiang ; Zeng, Liang ; Hong, Shaodong ; Huang, Yan ; Shao, Yang ; Xue, Jinhui ; Yang, Yunpeng
BACKGROUND:
TQ-B3139 is a novel ALK tyrosine kinase inhibitor (TKI) against a broad range of ALK mutations. The aim of this first-in-human phase I trial was to investigate the safety, tolerability, pharmacokinetics, and clinical efficacy of TQ-B3139 in ALK or ROS1 positive advanced NSCLC patients.
METHODS:
Following a 3 + 3 design, patients received escalating daily dose of TQ-B3139 (50-800 mg) continuously in 28-day cycles. Expansion stage started at dose of 200 mg twice daily (BID). The primary objectives were the safety, dose-limited toxicities (DLT) and recommended phase II dose (RP2D); secondary objectives included pharmacokinetics and antitumor activity. Non-obligatory tumor samples at baseline were collected and sequenced.
RESULTS:
The study enrolled 63 patients. Fifty-nine (93.4%) patients experienced treatment-related adverse events (TRAEs), mostly grade 1-2 vomiting (79.3%), diarrhea (76.1%) or nausea (68.2%). 1 (1/6) DLT occurred at 600 mg BID and 1 (1/3) at 800 mg BID. Based on safety and pharmacokinetics data, the RP2D was selected as 600 mg BID. At a dose level ≥200 mg BID, the overall response rate (ORR) was 76.7% (33/43), and the median progression free survival (mPFS) was 25.2 months (95%CI 11.9-NR) for TKI-naive patients. For TKI-treated patients, the ORR was 37.5% (6/16), and the mPFS was 5.4 months (95%CI 3.6-9.1). The ORR was 66.7% (2/3) in patients with ROS1 fusion at dose level ≥200 mg BID. In patients with measurable brain metastases, the intracranial ORR was 70% (7/10), with median intracranial PFS of 15.9 months. In TKI-treated patients, variant 3 and TP53 alteration were associated with poor PFS.
CONCLUSIONS:
TQ-B3139 was well-tolerated and exhibited promising anti-tumor activities in patients with ALK and ROS1 positive advanced NSCLC.
CLINICAL TRIAL NUMBER:
NCT03099330.
100 Deals associated with Envonalkib
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R&D Status
Approved
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| Indication | Country/Location | Organization | Date |
|---|---|---|---|
| ALK positive Non-Small Cell Lung Cancer | China | 11 Jun 2024 |
Developing
10 top R&D records. to view more data
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| Indication | Highest Phase | Country/Location | Organization | Date |
|---|---|---|---|---|
| MET gene amplification Non-small Cell Lung Cancer | Phase 2 | China | 11 Aug 2020 | |
| Advanced Malignant Solid Neoplasm | Phase 1 | China | 01 Feb 2021 | |
| Advanced cancer | Phase 1 | China | 12 Jul 2017 |
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Clinical Result
Clinical Result
Indication
Phase
Evaluation
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CTR20220526 (Pubmed) Manual  | Phase 1 | - | rnbtcqemfd(nkyqxusmqa) = iynxhvszum qctowkgism (wugljqysjs ) View more | Positive | 20 Mar 2024 | ||
NCT04009317 (Pubmed) Manual | Phase 3 | 264 | qjqaruwidl(ockbqnslwb) = elxicrjqop pdqlvlbsoq (yutcmojfbz, 15.64 - 30.36) View more | Positive | 14 Aug 2023 | ||
qjqaruwidl(ockbqnslwb) = wtgdjwiuea pdqlvlbsoq (yutcmojfbz, 8.28 - 13.73) View more | |||||||
Phase 3 | ALK positive Non-Small Cell Lung Cancer First line | 264 | Envonalkib 600mg (overall) | zhthaplaij(gptbmcfhnh) = wfthkxayst knwggsxrvn (kpddcxwbur ) View more | Superior | 03 Dec 2022 | |
(overall) | zhthaplaij(gptbmcfhnh) = laapyayzgz knwggsxrvn (kpddcxwbur ) View more | ||||||
Phase 1 | 63 | pmyuhjjgxq(nkrpuihyiz) = 76.1% rhbtudderv (jthtzstbxd ) View more | Positive | 05 Aug 2022 |
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