Discovery

Antengene is a science-driven company that seeks innovative therapeutic solutions to diseases and is keen on early discovery of transformative medicines. We have an experienced and creative drug discovery team with both outstanding industry and academic research experience, focusing on the discovery of first-in-class or best-in-class drugs. The drug modalities cover small molecule, monoclonal antibodies, antibody drug conjugates and bispecific antibodies. Our drug discovery aims to improve patient outcome as well as provide a prolonged survival with a better quality of life.

Pipeline

Assets

Target (Modality)

Regimen

Pre-clinical

Phase I

Phase II

Phase III

NDA

Commercialization

Antengene Rights

Partner

    ATG-010
    (Selinexor)1
  • XPO1
    (Small molecule)
  • Combo with dexamethasone (dex)
  • Combo with bortezomib and dex
  • Combo with IMiD/PI/anti-CD38 mAb and dex
  • Monotherapy
  • Combo with R-GDP
  • Combo with lenalidominde+rituximab
  • Combo with ICE/GemOx
  • Monotherapy
  • Monotherapy
  • Monotherapy
  • Monotherapy
  • Monotherapy
  • R/R Multiple Myeloma (MARCH)

    STORM
    (US and SK NDA approved)

  • R/R Multiple Myeloma (BENCH)

    BOSTON
    (US sNDA approved)

  • R/R and ND Multiple Myeloma (STOMP)

  • R/R Diffuse Large B-cell Lymphoma (SEARCH)

    SADAL (US sNDA approved)

  • R/R Diffuse Large B-cell Lymphoma (030 DLBCL)

  • R/R NHL (SWATCH)

  • R/R T-cell & NK/T-cell Lymphoma (TOUCH)

  • Non-small Cell Lung Cancer (TRUMP)*

  • Myelofibrosis (MF 035)

  • Maintenance Endometrial Cancer (SIENDO)

  • Advanced Liposarcoma (SEAL)

  • Recurrent Glioblastoma (KING)

    ATG-008
    (Onatasertib)
  • mTORC1/2
    (Small molecule)
  • Monotherapy
  • Combo with anti-PD-1 mAb
  • Monotherapy
  • Monotherapy
  • Combo with ATG-010 (Selinexor)
  • 2L+ HBV+ Hepatocellular Carcinoma (TORCH)

  • Advanced Solid Tumors and Hepatocellular Carcinoma (TORCH-2)*

  • Non-small Cell Lung Cancer (TRUMP)*

  • Advanced Solid Tumors (BUNCH)

  • R/R DLBCL (MATCH)

    ATG-016
    (Eltanexor)
  • XPO1
    (Small molecule)
  • Monotherapy
  • R/R MDS (HATCH) & Solid Tumors (REACH)

    MDS,CRC,PrC

    ATG-527
    (Verdinexor)
  • XPO1
    (Small molecule)
  • Monotherapy
  • Lupus,Anti-viral (i.e.,CAEBV) (CATCH)

    Healthy Volunteers

    ATG-019
    (KPT-9274)
  • PAK4/NAMPT
    (Small molecule)
  • Monotherapy ± niacin
  • Advanced Solid Tumors & NHL (TEACH)

    Solid
    Tumors

    ATG-017
    (AZD-0364)
  • ERK1/2
    (Small molecule)
  • Monotherapy
  • R/R Hem/Onc
    (ERASER)

ATG-017 (AZD-0364)

ATG-017 (AZD0364) is a potent and selective small molecule extracellular signal-regulated kinases 1 and 2 (ERK1/2) inhibitor currently under clinical development for the treatment of various solid tumors,non-Hodgkin lymphoma,acute myeloid leukemia (AML) and MM.

ERK1/2 are related protein-serine/threonine kinases that function as terminal kinases in the RAS-MAPK signal transduction cascade. This cascade regulates a large variety of cellular processes,including proliferation. The RAS-MAPK pathway is dysregulated in more than 30% of human cancers with the most frequent alterations being observed in RAS or BRAF genes across multiple tumor types. An ERK inhibitor enables the targeting of both RAS and BRAF mutant diseases. In nonclinical pharmacology studies,ATG-017 has demonstrated potent inhibition of ERK1/2 enzyme activity and tumor growth in vitro and in vivo.

We entered into a partnership with AstraZeneca in 2019 and obtained exclusive global rights to develop,commercialize and manufacture ATG-017. We are conducting a Phase I clinical trial for the treatment of advanced solid tumors and hematological malignancies in Australia. We plan to explore the combination of ATG-017 with ATG-012,ATG-008 (onatasertib),MEK inhibitors and immune checkpoint modulators,including ATG-101.

    ATG-1014
  • PD-L1/4-1BB
    (Bispecific)
  • Monotherapy
  • Hem/Onc
    (PROBE)

ATG-101

ATG-101 is a novel,PD-L1/CD137 (4-1BB) bi-specific antibody being developed for the treatment of hematological malignancies and solid tumors. Pre-clinical research showed that the therapeutic efficacy of ATG-101 is superior to that of the combination of PD-L1 and CD-137 antibodies,which may be attributable to ATG-101's ability to simultaneously bind tumor cells and T cells,leading to a potent tumor-localized T cell activation.

    ATG-037 5
  • CD73
    (Small molecule)
  • Monotherapy ± IO
  • Hem/Onc

ATG-037 5

ATG-037 is a highly potent,selective,orally-bioavailable small molecule inhibitor of CD73. It can reactivate antitumor immunity by inhibiting the highly immunosuppressive adenosine pathway.

CD73 is a rate-limiting enzyme that produces the highly immunosuppressive adenosine in the tumor microenvironment,thus leads to the immune escape of tumor cells. CD73 is expressed across a wide range of tumors and tumor infiltrating leukocytes,and often correlates with poor prognosis. Therefore,CD73 inhibition represents an effective approach in restoring antitumor immunity in caner patients. In addition,CD73 inhibition has great potential for combination with standard therapies or immune checkpoint inhibitors.

ATG-037 has demonstrated potent antitumor activity and a favorable safety profile in syngeneic animal models both as monotherapy and in combination with immune checkpoint inhibitors as well as chemotherapy,thus has great clinical potential either as a monotherapy or in combinations for the treatment of multiple tumor types.

    ATG-018
  • ATR
    (Small molecule)
  • Monotherapy
  • Hem/Onc

ATG-018

ATG-018 is a small molecule inhibitor targeting ataxia telangiectasia and Rad3 related (ATR) kinase being developed for the treatment of hematological malignancies and solid tumors.

    ATG-022
  • Claudin 18.2
    (ADC Targeting)
  • Monotherapy
  • Onc

ATG-022

ATG-022,an antibody drug conjugate targeting Claudin 18.2,is in the late pre-clinical research and GMP CMC stage.

    ATG-012
  • KRAS
    (Small molecule)
  • Monotherapy
  • Onc

ATG-012

ATG-012 is a KRAS G12C inhibitor against KRAS oncoprotein being developed for the treatment of solid tumors. Due to its unique MoA,it has the potential to be combined with many other therapies,including many of our own pipeline assets,such as ATG-017.

    ATG-031
  • CD24
    (Monoclonal antibody)
  • Monotherapy
  • Hem/Onc

ATG-031

ATG-031 is a potential first-in-class anti-CD24 monoclonal antibody being developed for the treatment of hematologic malignancies and solid tumors. ATG-031 potently stimulates macrophage-mediated phagocytosis and induces the destruction of cancer cells by blocking the 'Don't eat me' signals characterizing the growth of many cancers. In pre-clinical research, ATG-031 demonstrated single agent anti-tumor activity in animal models and showed synergy with chemotherapies,checkpoint inhibitors,and other therapeutic agents.

    ATG-027
  • B7H3/PD-L1
    (Bispecific)
  • Monotherapy
  • Hem/Onc

ATG-027

ATG-027 is a potential first-in-class bispecific antibody being developed for the treatment of hematologic malignancies and solid tumors. ATG-027 blocks the PD-1/PD-L1 interaction and the B7H3 interaction with its ligand to stimulate the activation of immune cells and mediates anti-tumor effect. ATG-027 also leads to the elimination of B7H3-positive tumor cells through ADCC/CDC effect. ATG-027 showed potent in vivo anti-tumor activity in mouse tumor models.

    ATG-032
  • LILRB
    (mAb)
  • Monotherapy
  • Hem/Onc

    ATG-041
  • Axl-Mer
    (Small molecule)
  • Monotherapy
  • Hem/Onc

  1.  Antengene Trials6

  2.  Partner Trials7

  3.  Registrational Trial in China

1 (s) NDA approved by US FDA, Greater China (mainland China, Hongkong, Taiwan), Australia, Singapore NDA submissions are completed; 2 Antengene has rights for Greater China (mainland China, Hong Kong, Taiwan, Macau), Australia, New Zealand, South Korea, and the ASEAN Countries; 3 Antengene has rights for Greater China, South Korea, Singapore, Malaysia, Indonesia, Vietnam, Laos, Cambodia, the Philippines, Thailand and Mongolia; 4 Licensed from Origincell and Antengene has obtained exclusive global rights to develop, commercialize and manufacture ATG-101; 5 Licensed from Calithera Biosciences and Antengene has obtained exclusive global rights to develop, commercialize and manufacture ATG-037; 6 Most advanced trial status in Antengene territories and the trials are responsible by Antengene; 7 Most advanced trial status in partner territories in the rest of the world and the trials are conducted by our licensing partners; * Investigator-initiated trials; R/R = relapsed/refractory; ND = newly diagnosed; MDS = myelodysplastic syndrome; CRC = colorectal cancer; PrC = prostate cancer; CAEBV = chronic active Epstein-Barr virus; NHL = non-Hodgkin lymphoma; Hem/Onc = hematological malignancies and solid tumors; SK= South Korea; R-GDP: Rituximab, Gemcitabine, Dexamethasone &Cisplatin; ICE = Ifosfamide, carboplatin, and etoposide; GemOx = Gemcitabine, oxaliplatin

  1. ATG-010 (Selinexor)1
  2. ATG-008 (Onatasertib)
  3. ATG-016 (Eltanexor)
  4. ATG-527 (Verdinexor)
  5. ATG-019 (KPT-9274)
  6. ATG-017 (AZD-0364)
  7. ATG-101
  8. ATG-037
  9. ATG-018
  10. ATG-022
  11. ATG-012
  12. ATG-031
  13. ATG-027
  14. ATG-032
  15. ATG-041