1. Effective PI3K/mTOR dual inhibitor.
(1) Blockage of PI3K/mTOR pathway decreases cell proliferation, playing an anti-tumor and anti-fibrosis role. The asset is able to inhibit four different subtypes of PI3K (α, β, γ, δ) kinase as well as mTOR kinase, so that the down-stream proteins function is affected by various degrees.
(2) The asset showed stronger PI3K (α, β, γ, δ) and mTOR inhibitory activity than competitor, and showed PI3K phosphorylated inhibitory activity in vitro.
2. Huge market for IPF.
(1) The total IPF patient population worldwide was 1.27 M in 2019, and Five-year survival rate from initial diagnosis of an Acute IPF is 18.4%, which is less than that of most cancers.
(2) Two marked drugs for IPF are limited effect with sever AEs and still unable to stop IPF progression. No drug has been recommended as Class I strategy for IPF in China.
(3) The asset phase 1 trial for IPF has been completed in the US.
3. Excellent for IPF treatment and prevention.
(1) The asset inhibited HFL1 cell proliferation in a nanomolar lever, much more effective than Pirfenidone and Nintedanib (micromolar level) for IPF in vitro.
(2) The asset showed better anti-fibrosis effect at 3 mg/kg/d dose than Pirfenidone (100 mg/kg/d) and Nintedanib (100 mg/kg/d) in vivo.
(3) For preventive treatment, the asset showed better anti-fibrosis effect at 0.75 mg/kg/d dose than Pirfenidone (100 mg/kg/d) and Nintedanib (100 mg/kg/d) in vivo.
4. High potential for anti-solid tumor.
(1) Only one PI3K/mTOR dual inhibitor: paxalisib is under phase 3 trial.
(2) The asset is in phase 1 clinical trial for solid tumor.
(3) The potential of asset to treat patients with PI3KCA-mut or PTEN-mut tumor is testing.
5. Effective for a variety of solid tumors.
(1) The asset strongly inhibited proliferation of tumor cells from multiplying tissue in a nanomolar lever.
(2) The asset showed better suppression of tumor growth than BKM120 at a 10-time less concentration (3 mg/kg/d) in HCC1954 (breast), PC3 (prostate) and NCI-H1975 (NSCLC) subcutaneous tumor model.
6. Good safety and phase 1 trial in China and US.
(1) hERG IC50/Free Cmax >50, 1mg/kg and all genotoxicity tests are negative in preclinical study.
(2) Oral administration for patients with advanced solid tumor (breast, colon, and neuroendocrine) phase 1 trial in China has been completed.
(3) No dose-related AEs and no SAE were found in the US phase 1 trial for IPF.
1. Asset type: PI3K/mTOR dual inhibitor
2. Indication: Idiopathic pulmonary fibrosis (IPF) and solid tumor, (FDA ODD）
3. Modality: Small molecular, FIC
4. Research phase: Phase 1
5. Cooperation demands: License-out or co-development
6. Research progress:
(1) IPF and solid tumor indications are in phase 1 trials.
(2) For IPF, the asset show better effective than Pirfenidone and Nintedanib at a less dose.
(3) For solid tumor, the asset show better effective than BKM120.
ComboX is a new brand of ACROBiosystems. ComboX products include our Streptavidin series products, coated plates, isotype controls for antibody and fusion protein drug research, and general-purpose antibodies.
Emerging VoCs, Omicron, Delta, Beta, Alpha mutants and so on, including RBD, S trimer, S1, NTD, NP, etc. These mutants are of high purity and bioactivity and can be used to evaluate the efficacy of the antibodies and vaccination.
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50+ targets designed for CAR detection, including PE/FITC/biotin labeled proteins. The key reagents for CD19 and BCMA were FDA DMF filed which can support your IND, NDA and BLA process.
GMP grade cytokines, reagents for cell activation, gene edition, DNA/RNA removal, etc. Particularly focus on product design, quality control and solution-based support to link each phase of your cell and gene therapy journey.
Full length multi-pass TPs with stabilized structure and high bioactivity for immunization, antibody screening, cell based assay and CAR detection, including hot CD20, Claudin 18.2， CD133, GPRC5D，CCR8, CCR5, etc.
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