The DOI matches its Crossref record; 22 of the 22 references it cites were found in a registry or an index.
Targeting CDK4/6 in patients with cancer
Open accessAbstract
The cyclin D-cyclin dependent kinase (CDK) 4/6-inhibitor of CDK4 (INK4)-retinoblastoma (Rb) pathway controls cell cycle progression by regulating the G1-S checkpoint. Dysregulation of the cyclin D-CDK4/6-INK4-Rb pathway results in increased proliferation, and is frequently observed in many types of cancer. Pathway activation can occur through a variety of mechanisms, including gene amplification or rearrangement, loss of negative regulators, epigenetic alterations, and point mutations in key pathway components. Due to the importance of CDK4/6 activity in cancer cells, CDK4/6 inhibitors have emerged as promising candidates for cancer treatment. Moreover, combination of a CDK4/6 inhibitor with other targeted therapies may help overcome acquired or de novo treatment resistance. Ongoing studies include combinations of CDK4/6 inhibitors with endocrine therapy and phosphatidylinositol 3-kinase (PI3K) pathway inhibitors for hormone receptor-positive (HR+) breast cancers, and with selective RAF and MEK inhibitors for tumors with alterations in the mitogen activated protein kinase (MAPK) pathway such as melanoma. In particular, the combination of CDK4/6 inhibitors with endocrine therapy, such as palbociclib's recent first-line approval in combination with letrozole, is expected to transform the treatment of HR+ breast cancer. Currently, three selective CDK4/6 inhibitors have been approved or are in late-stage development: palbociclib (PD-0332991), ribociclib (LEE011), and abemaciclib (LY2835219). Here we describe the current preclinical and clinical data for these novel agents and discuss combination strategies with other agents for the treatment of cancer.
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Citations
Cites
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Cited by
Ribociclib as first-line therapy for HR-positive, advanced breast cancer
Hortobagyi, G. N., Stemmer, S. M., Burris, H. A., Yap, Y.-S., Sonke, G. S., Paluch-Shimon, S., Campone, M., Blackwell, K. L., André, F., Winer, E. P., et al. (2016) · New England Journal of Medicine · doi:10.1056/nejmoa1609709 · Cited by 2,039
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The Cancer Genome Atlas Comprehensive Molecular Characterization of Renal Cell Carcinoma
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Genome-Informed Targeted Therapy for Osteosarcoma
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BackgroundMolecular mechanisms of resistance to CDK4/6 inhibitors in breast cancer: A review
Pandey, K., An, H., Kim, S. K., Lee, S. A., Kim, S., Lim, S. M., Kim, G. M., Sohn, J., & Moon, Y. W. (2019) · International Journal of Cancer · doi:10.1002/ijc.32020 · Cited by 361
Metadata
- Authors
- Hamilton, E., & Infante, J. R.
- Venue
- Cancer Treatment Reviews
- Publisher
- Elsevier BV
- Published
- 2016-04
- Volume
- 45
- Pages
- 129-138
- ISSN
- 0305-7372 (ISSN-L)
- OpenAlex
- W2295971206
- Cited by
- 481
- References
- 22
- FWCI
- 34.43
- Type
- journal article
- Language
- en
- Open access
- hybrid
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