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Last update 15 Nov 2025
Ankuilisi
Last update 15 Nov 2025
Overview
Basic Info
Drug Type Small molecule drug |
Synonyms H-012, IMM-H012, ZD-12 |
Target |
Action inhibitors |
Mechanism PI3K family inhibitors(Phosphatidylinositol 3-kinase family inhibitors) |
Therapeutic Areas |
Active Indication |
Inactive Indication- |
Originator Organization |
Active Organization |
Inactive Organization- |
License Organization- |
Drug Highest PhasePhase 1/2 |
First Approval Date- |
Regulation- |
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Related
1
Clinical Trials associated with AnkuilisiCTR20253468
一项评估安喹利司（IMM-H012）在晚期实体肿瘤患者中的安全性、耐受性、药代动力学特征和疗效的Ⅰ/Ⅱ期临床研究
[Translation] A Phase I/II clinical study evaluating the safety, tolerability, pharmacokinetic characteristics, and efficacy of Aquinlisone (IMM-H012) in patients with advanced solid tumors
100 Clinical Results associated with Ankuilisi
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100 Translational Medicine associated with Ankuilisi
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100 Patents (Medical) associated with Ankuilisi
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2
Literatures (Medical) associated with Ankuilisi01 Aug 2024BIOMEDICAL CHROMATOGRAPHY
Pharmacokinetics of IMM‐H012 in rats using ultra‐performance liquid chromatography‐tandem mass spectrometry
Article
Author: Jiang, Rongbin ; Zhu, Xia‐yin ; Wu, Shujuan ; Wu, Jialei ; Lin, Longquan ; Wen, Congcong ; Wang, Xianqin
Abstract:
The present study examined the pharmacokinetics of IMM‐H012 in rat plasma, utilizing ultra‐performance liquid chromatography‐tandem mass spectrometry (UPLC‐MS/MS). Internal standard cilostazol was employed, and plasma samples were processed using acetonitrile precipitation. A mobile phase (acetonitrile–0.1% formic acid in water) with gradient elution was used to achieve chromatographic separation using a UPLC BEH C18 column. In multiple reaction monitoring mode, electrospray ionization MS/MS was utilized in positive ionization mode. Based on findings, the lower limit of quantification was 2 ng/mL, and the linearity of IMM‐H012 in rat plasma was found to be acceptable within the range of 2–2000 ng/mL (R2 > 0.995). The intra‐day and inter‐day precision relative standard deviation was less than 14% of IMM‐H012 in rat plasma. The matrix effect was within the range of 102%–107%, and the accuracy ranged from 92% to 113%. Pharmacokinetics of IMM‐H012 in rats after oral administration were successfully studied using UPLC‐MS/MS.
25 May 2023Journal of medicinal chemistryQ1 · MEDICINE
Discovery of a Novel Class of PROTACs as Potent and Selective Estrogen Receptor α Degraders to Overcome Endocrine-Resistant Breast Cancer In Vitro and In Vivo.
Q1 · MEDICINE
Article
Author: Hu, Zhiye ; Lv, Junhui ; Huang, Yuan ; Deng, Xiangping ; Xie, Baohua ; Yin, Zhinang ; Du, Chuanqian ; Dong, Chune ; Liang, Kaiwei ; Li, Qiuzi ; Huang, Jian ; Zhou, Hai-Bing
The estrogen receptor (ER) is a well-established target for endocrine therapies of ER-positive breast cancer (ER+ BC), but endocrine resistance limits the efficacy of clinical drugs. Using proteolysis targeting chimera (PROTAC) technology to degrade ERα may be an effective alternative to endocrine therapies. Herein, we disclose a novel series of potent and selective ERα PROTACs based on an oxabicycloheptane sulfonamide (OBHSA) scaffold, with no associated ERβ degradation. These PROTACs showed significant antiproliferation and ERα degradation activities against a broad spectrum of ER+ BC cells including tamoxifen-resistant and ERα mutant cell lines. Genomics analysis confirmed that these PROTACs inhibited the nascent RNA synthesis of ERα target genes and impaired genome-wide ERα binding. Compound ZD12 exhibited excellent antitumor potency and ERα degradation activity in both tamoxifen-sensitive and -resistant BC mice models, which are superior to fulvestrant. This study demonstrates the potential of these PROTACs as novel drug candidates for endocrine-resistant BC treatment.
100 Deals associated with Ankuilisi
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R&D Status
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| Indication | Highest Phase | Country/Location | Organization | Date |
|---|---|---|---|---|
| Advanced Malignant Solid Neoplasm | Phase 2 | China | 26 Aug 2025 | |
| Advanced Malignant Solid Neoplasm | Phase 2 | China | 26 Aug 2025 |
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