Abemaciclib

Abemaciclib
Clinical data
Pronunciation	/əˌbɛməˈsaɪklɪb/; ə-BEM-ə-SY-klib
Trade names	Verzenio, Verzenios, Ramiven, others
Other names	LY2835219
AHFS/Drugs.com	Monograph
License data	US DailyMed: Abemaciclib;
Routes of; administration	By mouth
ATC code	L01EF03 (WHO) ;
Legal status
Legal status	AU: S4 (Prescription only); CA: ℞-only / Schedule D; US: ℞-only; EU: Rx-only;
Pharmacokinetic data
Bioavailability	45%
Protein binding	96.3%
Elimination half-life	18.3 hrs
Excretion	81% via feces, 3% via urine
Identifiers
	IUPAC name N-[5-[(4-Ethyl-1-piperazinyl)methyl]-2-pyridinyl]-5-fluoro-4-[4-fluoro-2-methyl-1-(1-methylethyl)-1H-benzimidazol-6-yl]-2-pyrimidinamine;
CAS Number	1231929-97-7;
PubChem CID	46220502;
DrugBank	DB12001;
ChemSpider	29340700;
UNII	60UAB198HK;
KEGG	D10688;
ChEMBL	ChEMBL3301610;
PDB ligand	6ZV (PDBe, RCSB PDB);
CompTox Dashboard (EPA)	DTXSID20673119 ;
ECHA InfoCard	100.233.787
Chemical and physical data
Formula	C27H32F2N8
Molar mass	506.606 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES CCN1CCN(CC1)Cc2ccc(nc2)Nc3ncc(c(n3)c4cc5c(c(c4)F)nc(n5C(C)C)C)F;
	InChI InChI=1S/C27H32F2N8/c1-5-35-8-10-36(11-9-35)16-19-6-7-24(30-14-19)33-27-31-15-22(29)25(34-27)20-12-21(28)26-23(13-20)37(17(2)3)18(4)32-26/h6-7,12-15,17H,5,8-11,16H2,1-4H3,(H,30,31,33,34); Key:UZWDCWONPYILKI-UHFFFAOYSA-N;

Abemaciclib, sold under the brand name Verzenio among others, is a medication for the treatment of advanced or metastatic breast cancers. It was developed by Eli Lilly and it acts as a CDK inhibitor selective for CDK4 and CDK6.^[4]

It was designated as a breakthrough therapy for breast cancer by the US Food and Drug Administration (FDA) in October 2015.^[5]

In September 2017, it was approved for use in the United States by the FDA for the treatment of certain breast cancers.^[6]

^ "Verzenio (Eli Lilly Australia Pty Ltd)". Therapeutic Goods Administration (TGA). 28 September 2022. Archived from the original on 18 March 2023. Retrieved 9 April 2023.
^ "Summary Basis of Decision (SBD) for Verzenio". Health Canada. 23 October 2014. Archived from the original on 31 May 2022. Retrieved 29 May 2022.
^ "Verzenios EPAR". European Medicines Agency. 27 September 2018. Retrieved 17 June 2024.
^ Lu J (August 2015). "Palbociclib: a first-in-class CDK4/CDK6 inhibitor for the treatment of hormone-receptor positive advanced breast cancer". Journal of Hematology & Oncology. 8 (1): 98. doi:10.1186/s13045-015-0194-5. PMC 4534142. PMID 26264704.
^ Digiulio S (8 October 2015). "FDA's Breakthrough Therapy Designation to Abemaciclib for Breast Cancer". Oncology Times. LWW Journals. Archived from the original on 4 June 2021. Retrieved 30 March 2016.
^ "FDA approves new treatment for certain advanced or metastatic breast cancers" (Press release). Food and Drug Administration. 28 September 2017. Archived from the original on 23 April 2019. Retrieved 29 September 2017.

[1] "Verzenio (Eli Lilly Australia Pty Ltd)". Therapeutic Goods Administration (TGA). 28 September 2022. Archived from the original on 18 March 2023. Retrieved 9 April 2023.

[2] "Summary Basis of Decision (SBD) for Verzenio". Health Canada. 23 October 2014. Archived from the original on 31 May 2022. Retrieved 29 May 2022.

[3] "Verzenios EPAR". European Medicines Agency. 27 September 2018. Retrieved 17 June 2024.

[4] Lu J (August 2015). "Palbociclib: a first-in-class CDK4/CDK6 inhibitor for the treatment of hormone-receptor positive advanced breast cancer". Journal of Hematology & Oncology. 8 (1): 98. doi:10.1186/s13045-015-0194-5. PMC 4534142. PMID 26264704.

[5] Digiulio S (8 October 2015). "FDA's Breakthrough Therapy Designation to Abemaciclib for Breast Cancer". Oncology Times. LWW Journals. Archived from the original on 4 June 2021. Retrieved 30 March 2016.

[FDA-approval-6] "FDA approves new treatment for certain advanced or metastatic breast cancers" (Press release). Food and Drug Administration. 28 September 2017. Archived from the original on 23 April 2019. Retrieved 29 September 2017.

[1]

[2]

[3]

[4]

[5]

[6]