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- Title
Ribociclib in HR+/HER2- Advanced or Metastatic Breast Cancer Patients.
- Authors
Rascon, Kaitlin; Flajc, Goran; De Angelis, Carmine; Liu, Xinli; Trivedi, Meghana V.; Ekinci, Ekim
- Abstract
<bold>Objective: </bold>To review the chemistry, pharmacology, pharmacokinetics, safety, and efficacy of ribociclib (LEE011, Kisqali) in hormone receptor-positive/human epidermal growth factor receptor-2-negative (HR+/HER2-) metastatic breast cancer.<bold>Data Sources: </bold>A PubMed search was performed using the terms 'Ribociclib', 'Kisqali', and 'LEE011' between May 2018 and November 2018. References of published articles and reviews were also assessed for additional information.<bold>Study Selection and Data Extraction: </bold>English-language preclinical and clinical studies on the chemistry, pharmacology, pharmacokinetics, safety, and efficacy of ribociclib were evaluated.<bold>Data Synthesis: </bold>Ribociclib, a cyclin-dependent kinase (CDK) 4/6 inhibitor, is Food and Drug Administration (FDA) approved in combination with endocrine therapy for treatment of HR+/HER2- advanced or metastatic breast cancer in premenopausal/perimenopausal and postmenopausal women. Three phase III trials have evaluated ribociclib in combination with endocrine therapy, including letrozole, anastrozole, tamoxifen, and fulvestrant. These studies found that ribociclib 600 mg/d, 21 days on, 7 days off, leads to a significantly greater median progression-free survival (PFS), ranging from 8 to 13 months. Ribociclib is well tolerated in elderly patients, maintains health-related quality of life, and significantly reduces pain scores. The dose-limiting toxicities found in phase I studies were neutropenia, thrombocytopenia, and QTc prolongation. Common adverse effects seen in phase III trials include neutropenia, leukopenia, nausea, diarrhea, vomiting, and fatigue. Relevance to Patient Care and Clinical Practice: Literature on the safety and efficacy of ribociclib as well as its place in therapy in comparison to other FDA-approved CDK4/6 inhibitors for breast cancer is discussed.<bold>Conclusions: </bold>Ribociclib, when added to endocrine therapy, significantly improves PFS and has manageable toxicity in premenopausal/perimenopausal and postmenopausal women with HR+/HER2- advanced breast cancer.
- Subjects
THERAPEUTIC use of antineoplastic agents; PROTEIN metabolism; AMINOPYRIDINES; BREAST tumors; CELL receptors; METASTASIS; PURINES; QUALITY of life; PERIMENOPAUSE; DISEASE progression
- Publication
Annals of Pharmacotherapy, 2019, Vol 53, Issue 5, p501
- ISSN
1060-0280
- Publication type
journal article
- DOI
10.1177/1060028018817904