Gozanertinib

CAS 1226549-49-0

MF C32H31N5O3 MW533.6 g/mol

(E)-4-(dimethylamino)-N-[3-[4-[[(1S)-2-hydroxy-1-phenylethyl]amino]-6-phenylfuro[2,3-d]pyrimidin-5-yl]phenyl]but-2-enamide

(2E)-4-(dimethylamino)-N-[3-(4-{[(1S)-2-hydroxy-1-phenylethyl]amino}-6-phenylfuro[2,3-d]pyrimidin-5-yl)phenyl]but-2-
enamide
epidermal growth factor receptor tyrosine kinase inhibitor, antineoplastic, DBPR 112, ABT 101, 6G0COS33K4

Gozanertinib (also known as DBPR112 or ABT-101) is an orally bioavailable, advanced small-molecule dual kinase inhibitor designed to treat advanced non-small cell lung cancer (NSCLC). It targets alterations in the epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor 2 (HER2) families.

Mechanism of Action

Gozanertinib is a furanopyrimidine-based tyrosine kinase inhibitor. It functions by entering the ATP-binding pocket of the receptor and forming an irreversible covalent bond with a specific cysteine residue (Cys797). By permanently blocking these receptors, it halts downstream oncogenic signaling pathways—specifically the RAS/RAF/MEK/ERK and PI3K/AKT cascades—thereby inducing cancer cell death and suppressing tumor expansion.

Target Profile and Key Mutations

Unlike earlier generations of tyrosine kinase inhibitors that only target standard configurations, gozanertinib is optimized to combat specific treatment-resistant mutations:

• EGFR Mutations: It effectively targets wild-type EGFR as well as the dual L858R/T790M resistance mutations.
• Exon 20 Insertions: A standout feature of gozanertinib is its preclinical potency against EGFR and HER2 exon 20 insertion (Ex20ins) mutations. According to chemical development findings published in the Journal of Medicinal Chemistry, it demonstrated ten times better potency against these specific insertions than the widely used third-generation inhibitor, osimertinib.

Development and Status

The drug was initially discovered through scaffold optimization by the National Health Research Institutes (NHRI) and is being co-developed with Anbogen Therapeutics. The International Nonproprietary Name (INN) “gozanertinib” was formally proposed for the compound in early 2025. Preclinical evaluations indicated favorable oral bioavailability and strong anti-tumor efficacy compared to older inhibitors like afatinib, advancing the compound into early-phase clinical trials

Gozanertinib is an orally bioavailable dual kinase inhibitor of epidermal growth factor receptor (EGFR; ErbB1) and human epidermal growth factor receptor 2 (HER2; EGFR2; ErbB2), including EGFR L858R, EGFR T790M and HER2 exon 20 insertion (Ex20ins) mutations, with potential antineoplastic activity. Upon oral administration, gozanertinib targets, binds to and inhibits the activity of EGFR or HER2 insertions or mutations. This prevents EGFR/HER2-mediated signaling, which may induce cell death and inhibit tumor growth in EGFR/HER2-overexpressing tumor cells. The ErbB receptor tyrosine kinase family is involved in key cellular functions, including cell growth and survival. EGFR and HER2 alterations constitutively upregulate kinase activity.

• Phase 1b/2 Study to Evaluate ABT-101 in Solid Tumor and NSCLC PatientsCTID: NCT05532696Phase: Phase 1/Phase 2Status: RecruitingDate: 2024-06-24
• A Study of DBPR112 in Patients With Head and Neck Cancer and EGFR Mutated Lung CancerCTID: NCT03246854Phase: Phase 1Status: TerminatedDate: 2020-12-17

PAT

https://patentscope.wipo.int/search/en/detail.jsf;jsessionid=253FEDD942539182DEE212A1132D1CB3.wapp1nB?docId=US442160569&_cid=P11-MQ1QBW-83342-1

PAT

https://patentscope.wipo.int/search/en/detail.jsf?docId=US43249513&_cid=P11-MQ1QG3-86325-1

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References

• Development of Furanopyrimidine-Based Orally Active Third-Generation EGFR Inhibitors for the Treatment of Non-Small Cell Lung CancerPublication Name: Journal of Medicinal ChemistryPublication Date: 2023-02-07PMCID: PMC9969398PMID: 36749735DOI: 10.1021/acs.jmedchem.2c01434
• Discovery of a Furanopyrimidine-Based Epidermal Growth Factor Receptor Inhibitor (DBPR112) as a Clinical Candidate for the Treatment of Non-Small Cell Lung CancerPublication Name: Journal of Medicinal ChemistryPublication Date: 2019-09-27PMID: 31560541DOI: 10.1021/acs.jmedchem.9b00722

PAT

• Active cancer immunotherapy by immune modulation via globo series antigensPublication Number: EP-4248214-A1Priority Date: 2020-11-19
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• Fused bicyclic and tricyclic pyrimidine compounds as tyrosine kinase inhibitorsPublication Number: US-8507502-B2Priority Date: 2008-11-10Grant Date: 2013-08-13
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• Active cancer immunotherapy through immune modulation via GLOBO series antigensPublication Number: CN-116847875-APriority Date: 2020-11-19
• Active cancer immunotherapy by immune modulation via globo series antigensPublication Number: CA-3200572-A1Priority Date: 2020-11-19
• Active cancer immunotherapy by immune modulation via globo series antigensPublication Number: WO-2022109601-A1Priority Date: 2020-11-19
• Active cancer immunotherapy by immune modulation via globo series antigensPublication Number: IL-302947-APriority Date: 2020-11-19
• Active cancer immunotherapy by immunomodulation through GLOBO family antigensPublication Number: KR-20230110529-APriority Date: 2020-11-19
• Crystalline forms of (s, e)-4-(dimethylamino)-n-(3-(4-(2-hydroxy-1-phenylethylamino)-6-phenylfuro[2,3-d]pyrimidin-5-yl)phenyl)but-2-enamide free basePublication Number: TW-I809967-BPriority Date: 2021-07-06Grant Date: 2023-07-21
• Crystalline forms of (S, E)-4-(dimethylamino)-N-(3-(4-(2-hydroxy-1-phenylethylamino)-6-phenylfuro[2,3-d]pyrimidin-5-yl)phenyl)but-2- enamide free basePublication Number: US-12240858-B2Priority Date: 2021-07-06Grant Date: 2025-03-04
• Active cancer immunotherapy by immune modulation via globo series antigensPublication Number: TW-202237177-APriority Date: 2020-11-19
• Active cancer immunotherapy by immune modulation via globo series antigensPublication Number: US-2024139301-A1Priority Date: 2020-11-19
• Active cancer immunotherapy by immune modulation via globo series antigensPublication Number: AU-2021382807-A1Priority Date: 2020-11-19
• Crystalline forms of (s, e)-4-(dimethylamino)-n-(3-(4-(2-hydroxy-1-phenylethylamino)-6-phenylfuro[2,3-d]pyrimidin-5-yl)phenyl)but-2-enamide free basePublication Number: US-2023021909-A1Priority Date: 2021-07-06
• Crystalline forms of (s, e)-4-(dimethylamino)-n-(3-(4-(2-hydroxy-1-phenylethylamino)-6-phenylfuro[2,3-d]pyrimidin-5-yl)phenyl)but-2-enamide free basePublication Number: WO-2023283269-A1Priority Date: 2021-07-06
• Crystalline forms of (s, e)-4-(dimethylamino)-n-(3-(4-(2-hydroxy-1-phenylethylamino)-6-phenylfuro[2,3-d]pyrimidin-5-yl)phenyl)but-2-enamide free basePublication Number: US-2024368175-A1Priority Date: 2021-07-06
• Crystalline forms of (s, e)-4-(dimethylamino)-n-(3-(4-(2-hydroxy-1-phenylethylamino)-6-phenylfuro[2,3-d]pyrimidin-5-yl)phenyl)but-2-enamide free basePublication Number: TW-202309041-APriority Date: 2021-07-06
• Crystalline forms of (s, e)-4-(dimethylamino)-n- (3-(4-(2-hydroxy-1-phenylethylamino)-6-phenylfuro[2,3-d]pyrimidin-5-yl)phenyl)but-2-enamide free basePublication Number: EP-4330259-A1Priority Date: 2021-07-06

//////gozanertinib, ANAX LABS, epidermal growth factor receptor tyrosine kinase inhibitor, antineoplastic, DBPR 112, ABT 101, 6G0COS33K4