China
Africa
Explore chapters and articles related to this topic
Small-Molecule Targeted Therapies
Published in David E. Thurston, Ilona Pysz, Chemistry and Pharmacology of Anticancer Drugs, 2021
Abemaciclib (VerzeniosTM) (Figure 6.77), developed by Eli Lilly, is a selective inhibitor of CDK4 and CDK6. It was designated a breakthrough therapy for breast cancer by the FDA in 2015, and was fully approved in 2017 both as a monotherapy and in combination with fulvestrant (FaslodexTM) for patients with (HR)-positive/(HER2)-negative advanced or metastatic breast cancer that has progressed after a hormone therapy or chemotherapy. In addition, in 2018 the FDA approved abemaciclib for use in combination with an aromatase inhibitor to treat postmenopausal women diagnosed with metastatic or advanced-stage (HR)-positive/(HER2)-negative breast cancer not yet treated with hormonal therapy.Structure of abemaciclib (VerzenioTM).
Breast cancer
Published in Peter Hoskin, Peter Ostler, Clinical Oncology, 2020
Palbociclib, ribociclib and abemaciclib (are small molecule inhibitors of cyclin-dependent kinases 4 and 6) they act by preventing DNA synthesis, blocking progression of the cell cycle from G1 to the S phase. They have shown exciting activity, and are now routinely used in combination with hormonal treatment in patients with metastatic ER+ disease.
Hormone Receptors and Endocrine Therapy in Breast Cancer
Published in Sherry X. Yang, Janet E. Dancey, Handbook of Therapeutic Biomarkers in Cancer, 2021
Sherry X. Yang, Nancy E. Davidson
Abemaciclib in combination with fulvestrant is approved after disease progression on endocrine therapy and prior chemotherapy, based on the MONARCH-2 trial [82]. Median PFS for patients taking abemaciclib with fulvestrant was 16.4 months compared to 9.3 months for those on placebo plus fulvestrant (HR 0.553, 95% CI, 0.449 to 0.681; P < 0.001). The most frequent adverse events of any grade were diarrhea, neutropenia, nausea, fatigue, and abdominal pain. The most frequently reported grade 3 or 4 adverse events in patients taking abemaciclib plus fulvestrant (>5%) were neutropenia, diarrhea, leukopenia, anemia, and infections. Additionally, abemaciclib is approved as monotherapy after progression with endocrine therapy and prior chemotherapy in the metastatic setting. It was based on MONARCH-1 a single-arm, open-label, multicenter study [83]. A total of 132 patients received oral 200 mg abemaciclib twice daily on a continuous schedule until disease progression or unmanageable toxicity. The objective response rate was 19.7%, with a median response duration of 8.6 months (95% CI, 5.8–10.2). The most common adverse events of any grade were diarrhea, fatigue, and nausea. Recently, abemaciclib in combination with an aromatase inhibitor was approved as initial endocrine-based therapy. The granted indication was based on the results from MONARCH-3. Abemaciclib plus endocrine therapy versus endocrine therapy alone extends PFS as first-line therapy [84]. Median PFS was 14.7 months for patients receiving endocrine therapy alone and was not reached for those with the combination treatment (HR 0.54, 95% CI, 0.41 to 0.72, P < 0.0001). This represents a 46% reduction in the risk of disease progression.
Cost-effectiveness of ribociclib versus palbociclib in combination with an aromatase inhibitor as first-line treatment of postmenopausal women with HR+/HER2− advanced breast cancer: analysis based on final OS results of MONALEESA-2 and PALOMA-2
Published in Journal of Medical Economics, 2023
David Cameron, Vikash Kumar Sharma, Chandroday Biswas, Cathy Clarke, David Chandiwana, Purnima Pathak
As mentioned above, another CDK4/6 inhibitor, abemaciclib, is also licensed and recommended for use in the same patient population as ribociclib and palbociclib in the UK21,45. A separate cost-effectiveness analysis of ribociclib versus abemaciclib has been conducted22, which also found ribociclib to be both cost-saving and cost-effective options as compared to abemaciclib. The results of these cost-effectiveness analyses have implications for the treatment of HR+/HER2− ABC in the UK, in which the CDK4/6 inhibitors ribociclib, palbocilib, and abemaciclib are all approved for use16,17,21. The results of both this analysis, and the separate analysis against abemaciclib, suggest that ribociclib is a cheaper and more effective treatment option compared with the other CDK4/6 inhibitors in the first-line endocrine setting.
Pharmacokinetic study on the co-administration of abemaciclib and astragaloside IV in rats
Published in Pharmaceutical Biology, 2022
Sen Sun, Lu Liu, Hongming Song, Hong Li
Traditional Chinese medicine has been widely used in clinic, especially in China. Except for cancer patients, some people received herbal treatments for anticancer therapy also increase the possibility of drug-drug interactions (Qi et al. 2015; Wang et al. 2020). Astragalus membranaeus (Fisch.) Bge. (Fabaceae) is a Chinese traditional medicinal plant with various pharmacological functions and has been used in the clinical treatment of breast cancer (Fu et al. 2014; Dong et al. 2022). As one of the most active ingredients of astragalus, astragaloside IV has been reported to suppress metastasis and tumour progression and enhanced the chemosensitivity of breast cancer (Jiang et al. 2017; Zheng et al. 2019; Hu et al. 2021). It is prescribed to breast cancer patients who received therapy of abemaciclib and influenced the pharmacokinetics and pharmacology of abemaciclib.
Review of cyclin-dependent kinase 4/6 inhibitors in the treatment of advanced or metastatic breast cancer
Published in Journal of Drug Assessment, 2021
Lakyn Husinka, Pamela H. Koerner, Rick T. Miller, William Trombatt
Financially, when evaluating the same patients from the PDC analysis, the patient out of pocket copay was highest for ribociclib patients with commercial insurance accompanied with commercial secondary or a prescription assistance program (PAP). However, in patients lacking a secondary payer, ribociclib had the lowest final copay. Patients on abemaciclib with a secondary payer had the lowest levels of final copay (Table 2). Additionally, 9% of patients had a zero dollar final copay. When reviewing the average copay of each patient’s first CDK 4/6 inhibitor dispense, palbociclib and abemaciclib had a lower out-of-pocket cost compared to the AWP of the medications at $68 and $83. The first fill average cost of ribociclib was more than 4x abemaciclib at $376. Although these products are expensive with an average 30 day average wholesale price (AWP) of $14,089 the final patient out-of-pocket cost is much lower.