pipeline
Pipeline

Best-in-class and First-in-Class small molecule therapeutics.

Program

Target(s)

Indication

1

2

3

4

5

6

7

Tumor immunology

ZX-101A

PI3Kδγ

Hematological Malignancies
Solid Tumors

ZX-101A is a next-generation of PI3Kδ/γ inhibitor with improved therapeutic window in pre-clinical models. ZX-101A doesn’t carry the purine motif common in Idelalisib & and Duvelisib and minimize the drug-drug interaction potential in combination therapies or in use with concomitant medications. Dual inhibition of PI3Kδ and PI3Kγ by ZX-101A as the treatment of hematologic malignancies may synergistically exert through directly inhibiting PI3K signaling in malignant lymphocytes and enhancing anti-tumor immunity. ZX-101A has the potential to be the best-in-class medicine for blood cancers as well as the first-in-class immune-oncology treatment to certain solid tumors.

The Phase I/IIa clinical trials for patients with relapsed/refractory solid tumors and hematological malignancies are ongoing in China and US.

ZX-4081

PI3Kδγ
Tumors

PI3Kγ is a molecular switch that controls immune suppression and activates integrin α4 and promotes immune suppressive myeloid polarization during tumor progression. It was demonstrated that inhibition of PI3Kγ overcomes resistance to checkpoint blockade therapy.

ZX-4081 is the most selective and potent PI3Kγ inhibitor up to date. In preclinical studies, it showed favorable pharmacokinetic profile and efficacy was confirmed in solid tumor models. ZX-4081 is on the way to become best-in-class PI3Kγ inhibitor for the treatment of solid tumors, either as single agent or combination with other anticancer agents.

ZX-4081 is currently in Phase I clinical trial development in the United States.

ZX-8177

ENPP1
Tumors

Ecto-nucleotide pyrophosphatase/phosphodiesterase-1 (ENPP1), has been discovered as the predominant enzyme hydrolyzing 2’3’-cGAMP, substrate of STING. ZX-8177 is a highly potent ENPP1 inhibitor which effectively induces IFN-β1 production and recruits M1 macrophages, NK cells and CD8+T cells to infiltrate the tumor immune microenvironment (TIME) to suppress tumor progression. In preclinical studies, ZX-8177 has exhibited synergistic anti-tumor effects in combination with conventional therapies such as chemo and radiotherapies, which may provide an effective cancer treatment overcoming the resistance and the common side effects.

ZX-8177 is currently in preclinical development and IND filing is scheduled in 2023.

ZX-5000

Undisclosed
Tumors

Targeted therapy

ZX-7101A

PA
Flu

ZX-7101A potently inhibits cap-dependent endonuclease (CEN) in the PA proteins of influenza A and B viruses. Its pharmacological property is suitable for a single dose to treat and prevent influenza A and B virus infections.

In preclinical studies, ZX-7101A demonstrated superior efficacy against anti-influenza virus over Oseltamivir, and comparable efficacy with Xofluza. Not like Xofluza, ZX-7101A showed no food effect on oral bioavailability, and potentially has better safety and efficacy in the clinic.

ZX-7101A is currently in Phase II clinical trial development in China.

ZX-9021

DHODH
Tumors

ZX-9021 is a novel and potent DHODH inhibitor which inhibits the abnormal proliferation and intracellular metabolism of tumor cells via de novo pyrimidine biosynthesis pathway. Preclinical studies have shown that ZX-9021 exhibited excellent anti-tumor efficacy through regulating cell growth and differentiation.

ZX-9021 is currently in preclinical development.

ZX-3000

Undisclosed
Tumors

Remarks
1:Optimization  2:Preclinical   3:IND    4:Phase I  5:Phase II   6:Phase III    7:Launched