(R)-1-(imidazo[1,2-a]pyridin-6-yl)ethan-1-amine hydrochloride cas 1841086-59-6

· CAS Number: 1841086-59-6
· Chemical Name: 4-((3-((2-((2,6-dichloro-3,5-dimethoxyphenyl)amino)-5-fluoropyrimidin-4-yl)amino)pyridin-2-yl)oxy)-N-methylpiperidine-1-carboxamide
· Common Code: TQ-B3101
· Main Targets: ALK (Anaplastic Lymphoma Kinase) and ROS1
· R&D Company: China Zhongda Tianqing Pharmaceutical Group
· Commercial Name: Anacitinib (Anaectinib), some sources refer to its commercial name as Selinixor, but be aware that this may be confusing with Selinexor used for treating multiple myeloma. "Anacitinib" is the more widely accepted name.
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Detailed Explanation
What is it?
TQ-B3101 (Anenakitin) is a novel, potent and highly selective oral small molecule tyrosine kinase inhibitor. Its mechanism of action is very similar to that of lorlatinib, and it also mainly targets the two key driver genes, ALK and ROS1, which play a crucial role in certain cancers.
2. Mechanism of Action
Its mechanism of action is similar to that of previous ALK inhibitors:
· Competitive inhibition: By competitively binding to the ATP binding sites within the kinase domains of ALK and ROS1, it inhibits the phosphorylation of the kinase.
· Blocking signaling pathways: Thus, it blocks the downstream key signaling pathways such as JAK/STAT, PI3K/AKT, and RAS/MEK/ERK.
· Inhibiting proliferation and inducing apoptosis: Ultimately, it inhibits the proliferation of tumor cells and induces their apoptosis (programmed cell death).
3. Key Features and Advantages
· Resistance design: Like lorlatinib, anerlitinib has also been designed to overcome resistance to the first and second generation ALK inhibitors (such as crizotinib and alectinib). It has inhibitory activity against various common ALK resistance mutations.
· Good blood-brain barrier penetration: Preclinical and clinical data show that anerlitinib can effectively penetrate the blood-brain barrier, which is crucial for controlling and treating the common central nervous system (CNS) metastases (i.e., brain metastases) of ALK-positive non-small cell lung cancer.
· Potential as a first-line treatment: Chinese clinical trials not only evaluated its efficacy in treated patients, but also conducted research as a first-line treatment option, and demonstrated excellent efficacy.
4. Clinical Application and Status
· Approval status: This drug was approved for marketing in China by the National Medical Products Administration (NMPA) in 2021.
· Indications: It is used for the treatment of patients with ALK-positive locally advanced or metastatic non-small cell lung cancer (NSCLC).
· Clinical data: The results of the key Phase II clinical study showed that anenatencin demonstrated a high objective response rate (ORR) both as a first-line treatment and for patients who had received crizotinib treatment, and it also showed significant efficacy for brain metastasis lesions.
5. Comparison with CAS 1270475-03-0 (Lorlatinib)
Both are potent inhibitors targeting ALK resistance and brain metastases, but there are some differences:
Properties: CAS 1841086-59-6 (Anenakitin/TQ-B3101) CAS 1270475-03-0 (Lorlatinib/PF-06463922)
Trade names: Anenakitin Lorbrena® (Lorlatinib)
Core targets: ALK, ROS1 ALK, ROS1
Key features: Overcomes drug resistance, highly effective against brain metastasis Overcomes drug resistance (especially G1202R), one of the strongest against brain metastasis
Status: One of the first-generation ALK inhibitors approved in China The first-generation ALK inhibitor globally
Market: Mainly targeted at the Chinese market, with price and accessibility advantages Global market, expensive
In simple terms, anerkitin can be regarded as the Chinese version of "loratadine". It is an important representative of China's achievement in "domestic substitution" and independent innovation in the field of precise oncology treatment, providing more and sometimes more cost-effective treatments for Chinese patients with ALK-positive lung cancer.