Mr. Ibrahem/Mobocertinib
Clinical data
Trade namesExkivity
Other namesTAK-788, AP-32788
AHFS/Drugs.comMonograph
License data
Pregnancy
category
Routes of
administration
By mouth
Drug classAntineoplastic
Legal status
Legal status
Identifiers
  • Propan-2-yl 2-(4-{[2-(dimethylamino)ethyl]methylamino}-2-methoxy-5-(prop-2-enamido)anilino)-4-(1-methyl-1H-indol-3-yl)pyrimidine-5-carboxylate
Chemical and physical data
FormulaC32H39N7O4
Molar mass585.709 g·mol−1
3D model (JSmol)
  • CC(C)OC(=O)C1=CN=C(N=C1C2=CN(C3=CC=CC=C32)C)NC4=C(C=C(C(=C4)NC(=O)C=C)N(C)CCN(C)C)OC
  • InChI=1S/C32H39N7O4/c1-9-29(40)34-24-16-25(28(42-8)17-27(24)38(6)15-14-37(4)5)35-32-33-18-22(31(41)43-20(2)3)30(36-32)23-19-39(7)26-13-11-10-12-21(23)26/h9-13,16-20H,1,14-15H2,2-8H3,(H,34,40)(H,33,35,36)
  • Key:AZSRSNUQCUDCGG-UHFFFAOYSA-N

  • as salt: InChI=1S/C32H39N7O4.C4H6O4/c1-9-29(40)34-24-16-25(28(42-8)17-27(24)38(6)15-14-37(4)5)35-32-33-18-22(31(41)43-20(2)3)30(36-32)23-19-39(7)26-13-11-10-12-21(23)26;5-3(6)1-2-4(7)8/h9-13,16-20H,1,14-15H2,2-8H3,(H,34,40)(H,33,35,36);1-2H2,(H,5,6)(H,7,8)
  • Key:YXYAEUMTJQGKHS-UHFFFAOYSA-N

Mobocertinib, sold under the brand name Exkivity, is a medication used to treat non-small cell lung cancer.[2] Specifically it is used for advanced cases with an epidermal growth factor receptor (EGFR) exon 20 insertion mutation.[2] It is taken by mouth once per day.[2]

Common side effects include diarrhea, rash, nausea, inflammation of the mouth, vomiting, decreased appetite, finger nail infections, tiredness, dry skin, and musculoskeletal pain.[2] Other side effects may include kidney problems, low potassium, pancreatitis, pneumonitis, and heart problems such as QTc prolongation.[2] Use in pregnancy may harm the baby.[2] It is a tyrosine kinase inhibitor that preferentially inhibits epidermal growth factor receptor (EGFR) bearing mutations in the exon 20 region.[5]

Mobocertinib was approved for medical use in the United States in 2021.[2] While it is available in the United Kingdom, it is not approved in Europe.[6] In the United Kingdom a month of medication costs the NHS about £7800 as of 2022.[6] In the United States this amount costs 24,600 USD.[7]

References

edit
  1. ^ a b "Exkivity APMDS". Therapeutic Goods Administration (TGA). 1 August 2022. Archived from the original on 2 August 2022. Retrieved 2 August 2022.
  2. ^ a b c d e f g h i j k l "Exkivity- mobocertinib capsule". DailyMed. Archived from the original on 1 October 2021. Retrieved 30 September 2021.
  3. ^ "Exkivity 40 mg hard capsules - Summary of Product Characteristics (SmPC)". (emc). 24 March 2022. Archived from the original on 25 March 2022. Retrieved 24 March 2022.
  4. ^ "FDA grants accelerated approval to mobocertinib for metastatic non-sma". U.S. Food and Drug Administration (FDA). 16 September 2021. Archived from the original on 16 September 2021. Retrieved 16 September 2021.   This article incorporates text from this source, which is in the public domain.
  5. ^ "Mobocertinib Monograph for Professionals". Drugs.com. Archived from the original on 3 July 2022. Retrieved 27 October 2022.
  6. ^ a b "Mobocertinib". SPS - Specialist Pharmacy Service. 28 March 2020. Archived from the original on 11 April 2022. Retrieved 27 October 2022.
  7. ^ "Exkivity Prices, Coupons, Copay & Patient Assistance". Drugs.com. Retrieved 27 October 2022.