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    Home > Active Ingredient News > Drugs Articles > With PI3Kα/δ dual inhibitor, CP Tianqing won its first breakthrough therapy!

    With PI3Kα/δ dual inhibitor, CP Tianqing won its first breakthrough therapy!

    • Last Update: 2021-08-10
    • Source: Internet
    • Author: User
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    On July 8, the CDE Breakthrough Therapy column was updated, and it was planned to include CP Tianqing’s TQ-B3525 as a breakthrough therapy

    TQ-B3525 is a new and selective oral PI3K α/δ inhibitor.

    PI3K, phosphatidylinositol 3-kinase, can be divided into three types: type I, type II, and type III.

    Currently, type I PI3K is widely studied.
    Studies have shown that this type of PI3K is closely related to tumors

    TQ-B3525 is a dual PI3K α/δ inhibitor.
    It can overcome the drug resistance caused by the up-regulation of PI3Kα subunit activity caused by PI3Kδ subunit inhibition alone, and at the same time significantly reduces toxic and side effects compared to PI3K pan-inhibitors

    Preclinical results showed that its inhibitory activity of PI3Kα and PI3Kδ was 41 and 138 times that of Buparlisib, respectively

    Currently, according to the Insight database, Tianqing has initiated 6 clinical trials in China, mainly for hematomas

    Among them, the two fastest progressing items have entered phase 2 clinical trials, targeting relapsed/refractory mantle cell lymphoma (MCL) and relapsed/refractory follicular lymphoma (FL)

    In terms of solid tumors, Tianqing also initiated a phase 1b clinical trial in combination with fulvestrant in the treatment of HR-positive and HER2-negative PIK3CA-mutated advanced breast cancer, and another for PI3KA mutation or PTEN deletion/low expression advanced bone tumors.
    Phase 1b clinical recruitment is underway

    TQ-B3525 Domestic clinical overview

    From the Insight database (http://db.


    At the 2020 ASCO meeting, Tianqing announced the clinical data of Phase 1 clinical trial (registration number: NCT03510767)

    This is a phase 1 clinical trial evaluating the safety, tolerability, pharmacokinetics, and anti-tumor activity of TQ-B3525 in the treatment of advanced malignant tumors in China.

    Patient baseline data

    From 2020 ASCO

    According to the 2014 Lugano classification, 23 lymphoma patients can be evaluated for clinical efficacy

    The total effective rate (ORR) was 60.
    9% (14/23, 4 cases of CR, 10 cases of PR), and the DCR was 87.
    0% (20/23)

    In terms of cancer types, for R/R FL patients (11 patients who had previously received rituximab treatment), the ORR was 72.
    7% (8/11, 2 patients with CR)

    For R/R MCL patients (2 patients who had previously received BTK inhibitor treatment), ORR was 100% (3/3)

    As of the data cutoff (2020.
    15), the median PFS of lymphoma patients had not reached (incident rate: 33.
    3%); the response duration of one FL patient reached 15.
    8 months at the data cutoff

    The efficacy data of TQ-B3525 in the treatment of hematoma

    From 2020 ASCO

    In terms of safety, a total of 39 patients (97.
    5%) had treatment-related AEs (TRAE), of which 12 cases (30%) were grade 3 or 4 TRAE

    The results show that TQ-B3525 can be tolerated in patients with advanced malignant tumors in China, and has shown promising anti-tumor activity in R/R lymphomas

    In China, there are already 25 PI3K inhibitors under development, including drugs that target different subunits of PI3K, as well as pan-PI3K inhibitors or dual-target inhibitors.
    However, no company has approved relevant products for the market, and the progress is the fastest Three of the products have been reported for production, including the PI3Kδ/γ inhibitor Duensibu introduced by CSPC, the PI3Kδ inhibitor Linpris from Yingli Pharmaceutical/Hengrui Medicine, and the PI3Kα/δ inhibitor Cupanisi from Bayer
    The difference between subunit selectivity and clinical development indications may be an important factor influencing product competitiveness in the future

    Nearly 3 billion R&D investment in 2020,

    60 projects to build an innovative drug pipeline

    Innovation is the lifeblood of an enterprise
    Nowadays, under the policy pressure and the intensified market competition, pharmaceutical companies have invested heavily in research and development.
    China's biopharmaceutical research and development investment has also increased year by year, reaching 2.
    853 billion yuan in 2020, accounting for approximately 12.
    1% of the total revenue that year , Ranked in the top five among domestic pharmaceutical companies

    According to the Insight database, Sino Biopharmaceuticals currently has a pipeline of 60 clinical-stage new drugs, most of which come from subsidiary Chia Tai Tianqing
    Among them, small-molecule chemical drugs are the main ones, with 45 small-molecule innovative drugs ready to be launched; 9 biosimilar drugs and 6 bio-innovative drugs are also quite competitive

    The fastest progress in chemical drugs is the ALK inhibitor TQ-B3139, which has started phase III clinical trials of head-to-head crizotinib.
    There are also multiple clinical studies of non-small cell lung cancer after crizotinib resistance to phase II
    CDK4/6 inhibitors, c-Met inhibitors, ROS1, etc.
    under development in the anti-tumor field have all progressed to phase II clinical trials

    Among them, the domestic CDK4/6 inhibitors of Eli Lilly and Pfizer’s pipercillil were approved for import in 2020 and 2018 respectively.
    The domestic Hengrui’s CDK4/6 inhibitors were the first to report for production, and Chia Tai Tianqing TQB3616 capsules and Fosun Pharma’s FCN-437c capsule followed closely behind
    In addition, Zhongsheng also deployed the third-generation EGFR inhibitor FHND9041 and the fourth-generation EGFR inhibitor TQB3804

    *Targets are organized according to official information, welcome to add in the comment area

    Tianqing’s closest bio-innovative drug to the market is Paimrizumab, which is co-operated with Kangfang Bio
    This PD-1 monoclonal antibody was initially reported for production in China in 2020.
    There are currently two indications for classic Hodgkin lymphoma (cHL) and first-line squamous NSCLC under review and are expected to be approved within this year; May this year , Paimrizumab has also taken an important step towards the sea: it submitted an NDA to the FDA

    Within the self-research pipeline, Tianqing has another PD-L1 monoclonal antibody TQB2450 in Phase III clinical trials
    This monoclonal antibody declared IND in 2017 and has initiated 18 clinical trials for more than ten cancer types including non-small cell lung cancer, triple negative breast cancer, head and neck squamous cell carcinoma, and cervical cancer
    In addition, Tianqing also deployed a number of promising targets: PD-L1/TGFβ double antibody, TIM-3 monoclonal antibody
    The value of these targets has been confirmed by clinical data from multinational pharmaceutical companies

    In terms of biosimilar drugs, China Biopharmaceuticals has 9 models under development
    Including the fiercely competitive adamu, bevaciz, rituximab, trastuzuma.
    the other 5 biosimilar drugs currently have no domestically produced similar drugs, and most of Tianqing belong to the first echelon


    Compared with innovative companies, Tianqing, as an established pharmaceutical company that combines imitation and innovation, started a little later than its peers in terms of innovative drugs.
    However, Tianqing's determination to transform innovation can be seen from the aspects of R&D investment and pipeline construction
    This breakthrough therapy identification is also a recognition of Tianqing’s innovative ability, which means that Tianqing’s innovative drug development has not only continued to increase in quantity, but also reached a new level in quality

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