Orelabrutinib

Drug for treatment of cancer

L01EL04 (WHO)

Legal statusLegal status

In general: ℞ (Prescription only)

Identifiers

IUPAC name

2-(4-Phenoxyphenyl)-6-(1-prop-2-enoylpiperidin-4-yl)pyridine-3-carboxamide

CAS Number

1655504-04-3

PubChem CID

91667513

IUPHAR/BPS

10629

DrugBank

DB16272

ChemSpider

82956396

UNII

WJA5UO9E10

ChEMBL

ChEMBL4650321

Chemical and physical dataFormulaC₂₆H₂₅N₃O₃Molar mass427.504 g·mol⁻¹3D model (JSmol)

Interactive image

SMILES

C=CC(=O)N1CCC(CC1)C2=NC(=C(C=C2)C(=O)N)C3=CC=C(C=C3)OC4=CC=CC=C4

InChI

InChI=1S/C26H25N3O3/c1-2-24(30)29-16-14-18(15-17-29)23-13-12-22(26(27)31)25(28-23)19-8-10-21(11-9-19)32-20-6-4-3-5-7-20/h2-13,18H,1,14-17H2,(H2,27,31)
Key:MZPVEMOYADUARK-UHFFFAOYSA-N

Orelabrutinib is a drug for the treatment of cancer.

In China, it is approved for patients with mantle cell lymphoma (MCL) and chronic lymphocytic leukemia/small lymphocytic lymphoma (CLL/SLL), who have received at least one treatment in the past.^[1]

Orelabrutinib is an inhibitor of Bruton's tyrosine kinase.^[2]

References

^ Dhillon S (March 2021). "Orelabrutinib: First Approval". Drugs. 81 (4): 503–507. doi:10.1007/s40265-021-01482-5. PMID 33704654.
^ Deng LJ, Zhou KS, Liu LH, Zhang MZ, Li ZM, Ji CY, et al. (August 2023). "Orelabrutinib for the treatment of relapsed or refractory MCL: a phase 1/2, open-label, multicenter, single-arm study". Blood Advances. 7 (16): 4349–4357. doi:10.1182/bloodadvances.2022009168. PMC 10432605. PMID 37078706.

Targeted cancer therapy / antineoplastic agents (L01)

CI monoclonal antibodies ("-mab")

Receptor tyrosine kinase	ErbB: HER1/EGFR (Cetuximab Panitumumab) HER2/neu (Pertuzumab, Trastuzumab (+hyaluronidase) Trastuzumab emtansine Trastuzumab deruxtecan)
Others for solid tumors	EpCAM (Catumaxomab Edrecolomab) VEGF-A (Bevacizumab)
Leukemia/lymphoma	lymphoid: CD3 (Glofitamab, Elranatamab, Mosunetuzumab), CD20 (Glofitamab Ibritumomab Mosunetuzumab Obinutuzumab Ofatumumab Rituximab Tositumomab), CD30 (Brentuximab), CD52 (Alemtuzumab) myeloid: CD33 (Gemtuzumab ozogamicin)
Other	Amivantamab Atezolizumab Avelumab Belantamab mafodotin Bermekimab Blinatumomab Cemiplimab Daratumumab Dinutuximab beta Dostarlimab Durvalumab Elotuzumab Enfortumab vedotin Epcoritamab Inotuzumab ozogamicin Ipilimumab Isatuximab Loncastuximab tesirine Mirvetuximab soravtansine Mogamulizumab Moxetumomab pasudotox Naxitamab Necitumumab Nivolumab Olaratumab Oportuzumab monatox Pembrolizumab Polatuzumab vedotin Prolgolimab Ramucirumab Retifanlimab Sabatolimab Sacituzumab govitecan Serplulimab Sugemalimab Tafasitamab Talquetamab Tarlatamab Teclistamab Tislelizumab Tisotumab vedotin Toripalimab Tremelimumab

Tyrosine kinase inhibitors ("-nib")

Receptor tyrosine kinase	ErbB: HER1/EGFR (Afatinib Aumolertinib Brigatinib Dacomitinib Erlotinib Gefitinib Icotinib Mobocertinib Olmutinib Osimertinib Rociletinib Vandetanib) HER1/EGFR and HER2/neu Lapatinib Neratinib Tucatinib RTK class III: C-kit and PDGFR (Avapritinib Axitinib Masitinib Pazopanib Ripretinib Sorafenib Sunitinib Toceranib) FLT3 (Lestaurtinib, Gilteritinib (AXL, ALK, LTK)) VEGFR Axitinib Cediranib Fruquintinib Lenvatinib Nintedanib Pazopanib Regorafenib Semaxanib Sorafenib Sunitinib Tivozanib Toceranib Vandetanib ALK Alectinib Brigatinib Ceritinib RET inhibitors: Entrectinib (ALK, ROS1, NTRK), Futibatinib (FGFR2), Infigratinib, Larotrectinib (NTRK), Pemigatinib (FGFR), Pralsetinib, Repotrectinib (ROS1, TRK, ALK), Selpercatinib (VEGFR, FGFR), Vandetanib (VEGFR, EGFR). c-MET inhibitors: Cabozantinib (VEGFR), Capmatinib, Crizotinib (ALK)
Non-receptor	bcr-abl Asciminib Bosutinib Dasatinib Imatinib Nilotinib Ponatinib Radotinib Src (Bosutinib Dasatinib) Janus kinase Baricitinib Fedratinib Filgotinib Lestaurtinib Momelotinib Pacritinib Ruxolitinib MAP2K Binimetinib Cobimetinib Selumetinib Trametinib EML4-ALK Crizotinib Entrectinib Lorlatinib Bruton's Acalabrutinib Ibrutinib Orelabrutinib Pirtobrutinib Zanubrutinib

Receptor tyrosine kinase