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Kinase Inhibitors in Preclinical Development – 2021

Insights on Preclinical Stage 220+ Kinase Inhibitors in Active Development

Team OmicsX by Team OmicsX
May 30, 2022
in Drug Targets, Kinase, Oncology, Pipeline, Small Molecules
Home Oncology Small Molecules Kinase
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First cancer targeting tyrosine kinase inhibitor imatinib was approved to enter the market by the US Food and Drug Administration (FDA) in 2001, since then an increasing number of small-molecule targeted drugs have been developed and approved for the treatment of cancer. By the end of June 2021, worldwide 96 small-molecule targeted antitumor drugs have been approved by the US FDA and the National Medical Products Administration (NMPA) of China, which majorly includes 73 kinase Inhibitors, beside other including Epigenetic Inhibitors, inhibitors of BCL-2, hedgehog pathway, proteasome, and PARP.

Global Oncology Intelligence Global Oncology Intelligence

Beside Cancer, nearly 14 other disease targeting small molecule Kinase Inhibitors were also approved worldwide during the same time period, thus making total tally to 87 approved kinase Inhibitors.

Despite great progress, small-molecule targeted anti-cancer drugs still face many challenges, such as a low response rate and drug resistance. This article carefully summarizes the approved cancer kinases inhibitors.

Check Also :-

  1. Upcoming Kinases Approvals their Competition & Market Size
  2. Kinases in Clinical Development – 200 Molecules / 200 Companies
  3. Kinases in Preclinical Development – 200 Molecules / 200 Companies
  4. Emerging Preclinical Stage Small Molecule Targeting Drug Developers. (131 Companies)
  5. Approved Non- Cancer Targeting Small Molecule Kinases.

Recently Approved Cancer Targeting Kinases Inhibitors (between 2019-2021)

wdt_ID SL No. Company Country Drug Code Target Stage Key Indication
1 1 Angex Pharmaceutical, Inc. United States AGX73 Multikinase IND Hepatocellular Carcinoma
2 2 Arrien Pharmaceuticals LLC United States ARN-3261 SIK2 / SIK3 IND Ovarian Cancer
3 3 Aucentra Therapeutics Pty Ltd Australia AU07 CDK9 IND Haematological Cancer
4 4 BioMed Valley Discoveries USA BVD-723 PI3Kγ IND Solid Tumor
5 5 Black Diamond Therapeutics USA BDTX-1535 EGFR IND Glioblastoma
6 6 FLAG Therapeutics, Inc. United States FLAG-003 VEGFR2, Tubulin IND Glioblastoma
7 7 Greenfire Bio LLC United States GRN-300 SIK2, SIK3 IND Ovarian Cancer
8 8 Immuneering Corporation United States IMM-1611441 RAF-MEK IND Solid Tumor
9 9 Meryx, Inc. United States MRX-2843 MerTK IND Acute Myeloid Leukemia
10 10 Petra Pharma Corporation USA PETRA 01 PIP4K2 IND Hematologic Cancers
11 11 PHusis Therapeutics, Inc. United States PHT-427 AKT/PDPK1 IND Cancer
12 12 Pyramid Biosciences Inc. United States PBI-200 TRK IND Solid Tumors
13 13 Shanghai YingLi Pharma China YL-15293 KRAS G12C IND Advanced Solid Tumor
14 14 Shenzhen TargetRx, Inc. China TGRX-326 ALK IND Non Small Cell Lung Cancer
15 15 Sierra Oncology, Inc. Canada SRA141 Cdc7 IND Advanced Solid Tumors
16 16 Stemline Therapeutics, Inc. USA SL-1001 RET IND Solid Tumors
17 17 Trethera Corporation United States TRE-515 Dck IND Myelodysplastic Syndrome
18 18 Turning Point Therapeutics USA TPX-0131 ALK IND Advanced Solid Tumor
19 19 1st Biotherapeutics Inc. South Korea 1 ST-201 Undisclosed Kinase Inhibitor Preclinical Solid Tumors
20 20 3D Medicines Co., Ltd. China 3D-011 VEGFR Preclinical Solid Tumors
21 21 ABM Therapeutics, Inc. China ABM-1383 MEK Preclinical Advanced Solid Tumors
22 22 ABM Therapeutics, Inc. China ABM-1381 Her2 Preclinical Advanced Solid Tumors
23 23 Adlai Nortye Biopharma China AN6025 HPK1 Preclinical Advanced Solid Tumors
24 24 AiViva BioPharma, Inc. United States AIV-001 VEGFR Preclinical Non-melanoma Skin Cancers
25 25 AiViva BioPharma, Inc. United States AIV-007 VEGFR, FGFR, PDGFR, TGF-β1 Preclinical Benign Prostatic Hyperplasia (BPH)
26 26 Allinky Biopharma Spain AIK4 RAS Preclinical Non-Small Cell Lung Cancer
27 27 Allomek Therapeutics LLC United States CIP-1374 MEK Preclinical Ovarian Cancer
28 28 Amplia Therapeutics Limited Australia AMP945 FAK Preclinical Solid Tumors
29 29 Amplia Therapeutics Limited Australia AMP886 FAK, VEGFR3, FLT3 Preclinical Solid Tumors
30 30 AnHeart Therapeutics Inc. China AB-329 / DS-1205 AXL Preclinical Non Small Cell Lung Cancer
31 31 Antengene Corporation China ATG-012 KRAS Preclinical Solid Tumor
32 32 Antengene Corporation China ATG-018 ATR Preclinical Solid Tumor
33 33 Apollomics, Inc. United States ABL-102 Multi Kinase Preclinical Solid Tumor
34 34 Apollomics, Inc. United States APL-103 EGRF Preclinical Solid Tumor
35 35 Applied Therapeutics, Inc. United States AT-104 PI3K δ/γ Preclinical Peripheral T-cell Lymphoma
36 36 Arjuna therapeutics United States Ag5 KRAS Preclinical Glioblastoma
37 37 Arjuna therapeutics United States Ag3 - Preclinical Lung Cancer
38 38 Arrien Pharmaceuticals LLC United States ARN-0953 MELK / Preclinical Acute Myeloid Leukemia
39 39 Arrien Pharmaceuticals LLC United States ARN-0894 Undisclosed Preclinical Cancer
40 40 Atrin Pharmaceuticals LLC United States ATRN-119 ATR Preclinical Solid Tumors
41 41 Aucentra Therapeutics Pty Ltd Australia AU3-14 CDK4/6 Preclinical Glioblastoma
42 42 Aucentra Therapeutics Pty Ltd Australia AU2-94 CDK4 Preclinical Cancer
43 43 Aucentra Therapeutics Pty Ltd Australia AU2-85 CDK8 Preclinical Cancer
44 44 Aucentra Therapeutics Pty Ltd Australia AU14-5 CDK2 Preclinical Cancer
45 45 Aucentra Therapeutics Pty Ltd Australia AU4-53 CDK9 / TRK Preclinical Cancer
46 46 AUM Biosciences Pte Ltd Singapore AUM001 / ETC-206 /ETC-1907206 MNK 1/2 Preclinical Solid Tumors
47 47 AUM Biosciences Pte Ltd Singapore AUM302 / IBL302 PIM/PI3K/mTOR Preclinical Solid Tumors
48 48 Avidin Ltd Hungary C-150 Multikinase, NFkB Preclinical Leukemia
49 49 Beta Pharma, Inc. USA BPI-1831 c-Met Preclinical Non-Small Cell Lung Cancer
50 50 BeyondSpring Pharma USA BPI-003 IKK Preclinical Solid Tumor
Company Country Drug Code Target Stage Key Indication
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Small Molecule Epigenetic Inhibitors – 2021

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Small Molecule Epigenetic Inhibitors – 2021

Small Molecule Cancer Therapies

  • Kinase Inhibitors – An Overview
    • Receptor Tyrosine Kinase Inhibitors
    • Non Receptor Tyrosine Kinase Inhibitors
    • Serine/Theonine Kinase Inhibitors
    • Approved Kinase Inhibitors
    • Kinase Inhibitors in Clinical Development
    • Kinase Inhibitors in Preclinical Development
    • Kinase Inhibitors – Clinical Drug Developers
    • Kinase Inhibitors – Preclinical Drug Developers
  • Epigenetic Inhibitors – An Overview
    • Approved Epigenetic Inhibitors
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