6-Amino-2-methylimidazo[1,2-a]pyridine-8-carbonitrile cas 2091732-43-1

The corresponding compound for CAS 2091732-43-1 is TTC-352. It is a selective partial agonist of the human estrogen receptor. It was originally developed by the University of Illinois in the United States and was licensed to TTC Oncology for clinical development (hence the name TTC-352), aiming to address the problem of resistance to existing endocrine therapies in hormone receptor-positive breast cancer.
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Chemical and physical properties
· IUPAC name: (E)-1-(2-(4-(1-(4-(2-(Dimethylamino)ethoxy)phenyl)-2-phenylbut-1-en-1-yl)phenoxy)ethyl) pyrrolidine
· Molecular formula: C₃₄H₄₄N₂O₂
· Molecular weight: 524.73 g/mol
· Structural features: TTC-352 is a benzothiophene analogue. It is structurally related to the well-known breast cancer drug tamoxifen, but has been optimized to possess unique pharmacological properties.
Mechanism of action
The mechanism of action of TTC-352 is extremely crucial and forms the basis for its differentiation from traditional endocrine therapy:
1. Target: Estrogen receptor
2. Mode of action: Selective estrogen receptor partial agonist/downregulator.
· It can bind to the estrogen receptor, but it does not activate it as strongly as natural estrogen does, thereby inhibiting the growth of estrogen-dependent tumor cells.
· More importantly, after binding to the receptor, it causes a unique conformational change in the receptor. This change makes the receptor unable to be effectively recruited by the co-activating proteins within the cell, and instead is more prone to be degraded by the proteasome.
· In simple terms, TTC-352 not only blocks the function of the estrogen receptor, but also promotes the body to clear (degrade) these receptor proteins themselves. This "downregulator" characteristic is particularly effective for cancer cells that have developed resistance to drugs such as tamoxifen.
Research Background and Application
· Indications: Primarily used for the treatment of hormone receptor-positive metastatic breast cancer, especially for patients who have developed resistance to standard endocrine therapies such as tamoxifen and/or aromatase inhibitors.
· Addressing Resistance Issues: Tamoxifen is a "selective estrogen receptor modulator" that exhibits agonist activity in certain tissues (such as the uterus), which may cause side effects (such as an increased risk of endometrial cancer) and lead to resistance. The design goal of TTC-352 is to maintain anti-cancer activity while reducing this agonist effect and overcoming the resistance mechanism by degrading the receptor.
Clinical development status
· Preclinical studies: In laboratory and animal models, TTC-352 demonstrated stronger anti-tumor activity than tamoxifen, and was able to effectively inhibit tumor growth resistant to tamoxifen.
· Phase I clinical trial: TTC-352 has completed the Phase I clinical trial. The main purpose of this stage was to evaluate the safety, tolerability, pharmacokinetics of the drug in the human body, and to determine the recommended dosage.
· Trial identifier: NCT03574228
· Status: Completed.
· Results: Preliminary data show that TTC-352 exhibited acceptable safety and tolerability characteristics in patients with advanced breast cancer, and showed initial signs of anti-tumor activity, providing a basis for subsequent studies.
At present, there are no widely publicized latest developments regarding the subsequent development status of this compound (such as whether it has entered the Phase II clinical trial). The research and development may be suspended or redirected due to various factors (such as funds, strategic adjustments, or efficacy data).
Summary

· CAS 2091732-43-1 (TTC-352) is a breast cancer candidate drug with an innovative mechanism of action.
· Its core value lies in its estrogen receptor down-regulator property, providing a promising new strategy for overcoming endocrine therapy resistance.
· Although the I-phase clinical trial has been successfully completed, demonstrating its basic safety and feasibility, the future development and marketing of this drug still await further clinical research results and the company's development decisions.