Enozertinib

CAS 2489185-38-6

MF C35H42F2N8O3 MW660.8

N-[2-[4-(4-cyclopropylpiperazin-1-yl)piperidin-1-yl]-5-[[6-[(3R)-3-(3,5-difluorophenyl)-1,2-oxazolidin-2-yl]pyrimidin-4-yl]amino]-4-methoxyphenyl]prop-2-enamide

• N-(2-(4-(4-cyclopropylpiperazine-1-yl)piperidine-1-yl)-5-((6-((R)-3-(3,5-difluorophenyl)isoxazolidine-2-yl)pyrimidine-4-yl)amino)-4-methoxyphenyl)acrylamide
• N-[2-[4-(4-Cyclopropyl-1-piperazinyl)-1-piperidinyl]-5-[[6-[(3R)-3-(3,5-difluorophenyl)-2-isoxazolidinyl]-4-pyrimidinyl]amino]-4-methoxyphenyl]-2-propenamide
• N-[2-[4-(4-cyclopropylpiperazin-1-yl)piperidin-1-yl]-5-[[6-[(3R)-3-(3,5-difluorophenyl)-1,2-oxazolidin-2-yl]pyrimidin-4-yl]amino]-4-methoxyphenyl]prop-2-enamide

epidermal growth factor receptor tyrosine kinase inhibitor, antineoplastic, ORIC-114, ORIC 114, DU24UP8R94

Enozertinib (formerly ORIC-114) is an investigational, orally bioavailable, and brain-penetrant dual EGFR/HER2 inhibitor developed by ORIC Pharmaceuticals. It targets cancers with exon 20 insertion and atypical EGFR mutations. Its core profile highlights its ability to cross the blood-brain barrier.

How it Works

Enozertinib acts as an irreversible, mutant-selective covalent inhibitor. By blocking overactive EGFR and HER2 signaling, it induces cell death and inhibits tumor growth. Because it penetrates the central nervous system (CNS), it is uniquely suited to treat both primary brain tumors and brain metastases—a common complication in non-small cell lung cancer (NSCLC).

Enozertinib is an orally bioavailable, central nervous system (CNS) penetrating, mutant-selective covalent inhibitor of epidermal growth factor receptor (EGFR; ErbB1) and human epidermal growth factor receptor 2 (HER2; EGFR2; ErbB2) alterations, including exon 20 insertion (Ex20ins) mutations, with potential antineoplastic activity. Upon oral administration, enozertinib selectively targets, irreversibly binds to and inhibits the activity of EGFR or HER2 insertions or mutations. This prevents EGFR/HER2-mediated signaling. This may induce cell death and inhibit tumor growth in EGFR/HER2-overexpressing tumor cells. Enozertinib is able to penetrate the blood-brain-barrier (BBB) and may therefore exert its activity against EGFR Ex20ins-driven CNS primary tumors and CNS metastases. 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.

SYN

https://drughunter.com/molecule/enozertinib-oric-114

SYN

[US11466000B2]

https://patentscope.wipo.int/search/en/detail.jsf?docId=US353221168&_cid=P11-MPAL9B-17125-1

PAT

https://patentscope.wipo.int/search/en/detail.jsf?docId=WO2020190119&_cid=P11-MPAL1R-09757-1

SIMILAR SYNTHESIS

ADVT

ANAX LABORATORIES

WEBSITE https://www.anaxlab.com/

Discovery Solutions, Supporting the chemistry needs of clients in the Medical, Analytical and Bio Sciences

Development Solutions, Developing from Lab scale to PR&D, Kilo Scale-ups and Commercial Scales

SEE MORE………Integrated Solutions, Manufacturing Solutions, Products,
Can’t Find? Let’s Connect

Phone : +91 897704 2010 /  +91 9177075735, Email : info@anaxlab.com

#MedicinalChemistry, #DrugDiscovery, #OrganicSynthesis, #ChemicalLibrary, #BuildingBlocks, #SARStudies, #ChemistryInnovation, #medchem, #Drugdevelopment, #Biotech, #Biotechnology, #AnaxLaboratories, #Pharma

AS ON FEB2026 4.574 LAKHS VIEWS ON BLOG WORLDREACH AVAILABLEFOR YOUR ADVERTISEMENT

join me on Linkedin

Anthony Melvin Crasto Ph.D – India | LinkedIn

join me on Researchgate

RESEARCHGATE

join me on Facebook

Anthony Melvin Crasto Dr. | Facebook

• Twitter
• FACEBOOK

join me on twitter

Anthony Melvin Crasto Dr. | twitter

+919321316780 call whatsaapp

EMAIL. amcrasto@gmail.com

References

• Egfr inhibitor for treating cancers comprising atypical egfr mutationsPublication Number: WO-2024233313-A1Priority Date: 2023-05-05
• Fumarate, tartrate, malate, and citrate salts of an egfr inhibitorPublication Number: WO-2024096624-A1Priority Date: 2022-11-03
• Malonate and glycolate salts of an egfr inhibitorPublication Number: WO-2024097848-A1Priority Date: 2022-11-03
• Malonate and glycolate salts of an egfr inhibitorPublication Number: EP-4611902-A1Priority Date: 2022-11-03
• Fumarate, tartrate, malate, and citrate salts of an egfr inhibitorPublication Number: EP-4612147-A1Priority Date: 2022-11-03
• Fumarate, tartrate, malate and citrate salts of EGFR inhibitorsPublication Number: CN-120035590-APriority Date: 2022-11-03
• Heteroaryl derivative, method for producing same, and pharmaceutical composition comprising same as effective componentPublication Number: US-11466000-B2Priority Date: 2019-03-19Grant Date: 2022-10-11
• Heteroaryl derivatives, their preparation methods, and pharmaceutical compositions containing them as active ingredientsPublication Number: CN-115838369-APriority Date: 2019-03-19
• Heteroaryl derivatives, methods for their preparation, and pharmaceutical compositions containing them as active ingredientsPublication Number: CN-114605400-APriority Date: 2019-03-19
• HETEROARYL DERIVATIVE, METHOD FOR PRODUCING THE SAME, AND PHARMACEUTICAL COMPOSITION INCLUDING THE SAME AS AN EFFECTIVE COMPONENTPublication Number: BR-112021018704-B1Priority Date: 2019-03-19
• Heteroaryl derivative, method for producing same, and pharmaceutical composition comprising same as effective componentPublication Number: US-2022289733-A1Priority Date: 2019-03-19
• Heteroaryl derivatives, methods for producing heteroaryl derivatives, and pharmaceutical compositions containing heteroaryl derivatives as active ingredientsPublication Number: JP-7394298-B2Priority Date: 2019-03-19Grant Date: 2023-12-08
• Heteroaryl derivatives, methods for their preparation, and pharmaceutical compositions containing them as active ingredientsPublication Number: CN-113993866-APriority Date: 2019-03-19

//////////enozertinib, anax labs, epidermal growth factor receptor tyrosine kinase inhibitor, antineoplastic, ORIC-114, ORIC 114, DU24UP8R94