Abemaciclib (Verzenio™) is an orally administered inhibitor of cyclin-dependent kinases 4 and 6 that is being developed by Eli Lilly and Company. Abemaciclib has been approved in the USA for the treatment of hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative advanced or metastatic breast cancer, in combination with fulvestrant in women with disease progression following endocrine therapy, and as monotherapy in adult patients with disease progression following endocrine therapy and prior chemotherapy in the metastatic setting. In addition, abemaciclib is in various stages of development internationally for a variety of cancers. This article summarizes the milestones in the development of abemaciclib leading to its first approval for the treatment of patients with HR-positive, HER2-negative advanced or metastatic breast cancer.
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Adis Insight. Drug profile: abemaciclib. 2017. http://www.adisinsight.springer.com. Accessed 13 Oct 2017.
Xu H, Yu S, Liu Q, et al. Recent advances of highly selective CDK4/6 inhibitors in breast cancer. J Hematol Oncol. 2017. https://doi.org/10.1186/s13045-017-0467-2.
Eli Lilly and Company. VERZENIO™ (abemaciclib): US prescribing information. 2017. https://www.fda.gov. Accessed 17 Oct 2017.
US FDA. FDA approves new treatment for certain advanced or metastatic breast cancers [media release]. 28 Sep 2017. https://www.fda.gov.
Kwapisz D. Cyclin-dependent kinase 4/6 inhibitors in breast cancer: palbociclib, ribociclib, and abemaciclib. Breast Cancer Res Treat. 2017. https://doi.org/10.1007/s10549-017-4385-3.
Patnaik A, Rosen LS, Tolaney SM, et al. Efficacy and safety of abemaciclib, an inhibitor of CDK4 and CDK6, for patients with breast cancer, non-small cell lung cancer, and other solid tumors. Cancer Discov. 2016;6(7):740–53.
Eli Lilly and Company. FDA grants priority review for potential new indication for Lilly’s Verzenio™ (abemaciclib) as initial treatment of advanced breast cancer [media release]. 12 Oct 2017. https://www.lilly.com.
Eli Lilly. Lilly and AstraZeneca expand immuno-oncology research collaboration with new combinations [media release]. 22 Oct 2015. https://www.lilly.com/.
Eli Lilly. Lilly and Merck expand immuno-oncology collaboration adding abemaciclib and KEYTRUDA® combination trial [media release]. 10 Dec 2015. https://www.lilly.com/.
Finn RS, Aleshin A, Slamon DJ. Targeting the cyclin-dependent kinases (CDK) 4/6 in estrogen receptor-positive breast cancers. Breast Cancer Res. 2016. https://doi.org/10.1186/s13058-015-0661-5.
Urruticoechea A, Smith IE, Dowsett M. Proliferation marker Ki-67 in early breast cancer. J Clin Oncol. 2005;23(28):7212–20.
Hurvitz S, Martin M, Fernandez Abad M, et al. Biological effects of abemaciclib in a phase 2 neoadjuvant study for post-menopausal patients with HR+, HER2-breast cancer [abstract no. S4-06]. Cancer Res. 2017;77(4 Suppl).
Hurvitz S, Abad MF, Rostorfer R, et al. Interim results from neoMONARCH: a neoadjuvant phase II study of abemaciclib in postmenopausal women with HR +/HER2-breast cancer (BC) [abstract no. LBA13]. Ann Oncol. 2016;27(Suppl 6).
Goodman A. Abemaciclib plus anastrozole: promising signals reported in phase II study of early breast cancer. 2017. http://www.ascopost.com Accessed 2 Nov 2017.
Fujiwara Y, Tamura K, Kondo S, et al. Phase 1 study of abemaciclib, an inhibitor of CDK 4 and 6, as a single agent for Japanese patients with advanced cancer. Cancer Chemother Pharmacol. 2016;78(2):281–8.
AstraZeneca Pharmaceuticals. FASLODEX® (fulvestrant) injection: US prescribing information. 2017. https://www.fda.gov. Accessed 1 Nov 2017.
Sledge GW Jr, Toi M, Neven P, et al. MONARCH 2: abemaciclib in combination with fulvestrant in women with HR+/HER2− advanced breast cancer who had progressed while receiving endocrine therapy. J Clin Oncol. 2017;35(25):2875–84.
Dickler MN, Tolaney SM, Rugo HS, et al. MONARCH 1, a phase II study of abemaciclib, a CDK4 and CDK6 inhibitor, as a single agent, in patients with refractory HR+/HER2− metastatic breast cancer. Clin Cancer Res. 2017;23(17):5218–24.
Rugo H, Nanda S, Koustenis A. Subgroup analysis by prior treatment and disease burden in MONARCH 1: a phase 2 study of monotherapy abemaciclib, a CDK4 & 6 inhibitor, in patients with HR+/HER2 metastatic breast cancer (MBC) following chemotherapy [abstract no. P6-11-12]. Cancer Res. 2017;77(4 Suppl).
Goetz MP, Toi M, Campone M, et al. MONARCH 3: abemaciclib as initial therapy for advanced breast cancer. J Clin Oncol. 2017. https://doi.org/10.1200/jco.2017.75.6155.
Tolaney SM, Lin NU, Thornton D, et al. Abemaciclib for the treatment of brain metastases (BM) secondary to hormone receptor positive (HR+), HER2 negative breast cancer [abstract no. 1019]. J Clin Oncol. 2017;35(15 Suppl).
US National Library of Medicine. Clinicaltrials.gov. 10 Oct 2017. https://clinicaltrials.gov. Accessed 12 Oct 2017.
Eli Lilly and Company. Lilly reports topline results from phase 3 JUNIPER trial evaluating Verzenio™ (abemaciclib) in KRAS-mutated, advanced non-small cell lung cancer [media release]. 10 Oct 2017. https://www.lilly.com.
Goldman JW, Shi P, Reck M, et al. Treatment rationale and study design for the JUNIPER study: a randomized phase III study of abemaciclib with best supportive care versus erlotinib with best supportive care in patients with stage IV non-small-cell lung cancer with a detectable KRAS mutation whose disease has progressed after platinum-based chemotherapy. Clin Lung Cancer. 2016;17(1):80–4.
The preparation of this review was not supported by any external funding.
Conflicts of interest
During the peer review process the manufacturer of the agent under review was offered an opportunity to comment on the article. Changes resulting from any comments received were made by the authors on the basis of scientific completeness and accuracy. Esther Kim is a salaried employee of Adis/Springer, is responsible for the article content and declares no relevant conflicts of interest.
Additional information about this Adis Drug Review can be found at http://www.medengine.com/Redeem/3BCCF0602F7F3723.
This profile has been extracted and modified from the AdisInsight database. AdisInsight tracks drug development worldwide through the entire development process, from discovery, through pre-clinical and clinical studies to market launch and beyond.
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Kim, E.S. Abemaciclib: First Global Approval. Drugs 77, 2063–2070 (2017). https://doi.org/10.1007/s40265-017-0840-z