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The cell-cycle regulatory proteins CDK4 and CDK6 drive progression through the G1–S phase transition, a checkpoint in preventing abnormal cell proliferaition.1,2 Uncontrolled cell division caused by the dysregulated activation of CDK4/6 is common in cancer.Gene deletion, mutation, or promoter hypermethylation leading to the loss of INK4 inhibitors can cause the overactivation of CDK4/6.3
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CDK4/6 Inhibitors
CDK4/6 inhibitors target enzymes CDK4 and CDK6, interrupting signals that stimulate the proliferation of cancer cells. This table outlines CDK4/6 inhibitors both approved by the FDA and in the pipeline.
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CDK4/6 Inhibitors Approved by the FDA |
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Brand Name (Generic Drug Name) |
Indications |
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Verzenio (abemaciclib)1 |
Treatment of adult patients with HR-positive, HER2-negative node-positive, early breast cancer at high risk of recurrence in combination with endocrine therapy (tamoxifen or an aromatase inhibitor) |
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Treatment of adult patients with HR-positive, HER2-negative advanced or metastatic breast cancer in combination with an aromatase inhibitor as initial endocrine-based therapy |
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Treatment in combination with fulvestrant for adult patients with HR-positive, HER2-negative advanced or metastatic breast cancer with disease progression following endocrine therapy |
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Treatment as monotherapy for adult patients with HR-positive, HER2-negative advanced or metastatic breast cancer with disease progression following endocrine therapy and prior chemotherapy in the metastatic setting |
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Kisqali (ribociclib)2 |
Treatment of adult patients with HR-positive, HER2-negative advanced or metastatic breast cancer in combination with an aromatase inhibitor as initial endocrine-based therapy |
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Treatment of adult patients with HR-positive, HER2-negative advanced or metastatic breast cancer in combination with fulvestrant as initial endocrine-based therapy or following disease progression on endocrine therapy in postmenopausal women or in men |
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Ibrance (palbociclib)3 |
Treatment of adult patients with HR-positive, HER2-negative metastatic breast cancer in combination with an aromatase inhibitor as the first hormonal based therapy |
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Treatment of adult patients with HR-positive, HER2-negative metastatic breast cancer in combination with fulvestrant in patients with disease progression following hormonal therapy |
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Cosela (trilaciclib)4 |
Treatment to decrease the incidence of chemotherapy-induced myelosuppression in adult patients with extensive-stage SCLC when administered prior to a platinum/etoposide-containing regimen or topotecan-containing regimen |
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CDK4/6 Inhibitors in the Pipeline |
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Trilaciclib4 |
Treatment is being evaluated in triple-negative breast cancer and metastatic urothelial carcinoma |
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Lerociclib5 |
Treatment is being evaluated in metastatic breast cancer |
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Dalpiciclib6 |
Treatment is being evaluated in advanced breast cancer |
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HR, hormone receptor; HER2, human epidermal growth factor receptor 2; SCLC, small cell lung cancer |
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