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Chemical Compound Review

Palbociclib     10-cyclopentyl-8-ethanoyl-7- methyl-3-[(5...

Synonyms: PubChem16671, QCR-200, Kinome_3823, Kinome_3824, S1116_Selleck, ...
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Disease relevance of PD 0332991

  • PD 0332991, therefore, represents the first promising and specific inhibitor for therapeutic targeting of Cdk4/6 in multiple myeloma and possibly other B-cell cancers [1].
  • PD 0332991 warrants phase II testing at 125 mg once daily, at which dose neutropenia was the sole significant toxicity [2].
  • In this article, we review the development of palbociclib and its use in treatment of hormone receptor-positive metastatic breast cancer in the context of other FDA-approved agents in this setting [3].

High impact information on PD 0332991

  • Inhibition of Cdk4/6 by PD 0332991 is not accompanied by induction of apoptosis [1].
  • Here, we show that by specific inhibition of Cdk4/6, the orally active small-molecule PD 0332991 potently induces G(1) arrest in primary bone marrow myeloma cells ex vivo and prevents tumor growth in disseminated human myeloma xenografts [1].
  • C2C12 myoblasts maintained in mitogen-rich media and exposed to a Cdk4/Cdk6 inhibitor PD 0332991 accumulated in G(1) cell cycle phase [4].
  • Consistent with a role for Cdk4/Cdk6 activity as a regulator of myogenic differentiation, we observed that PD 0332991 exposure promoted morphologic changes and enhanced the expression of muscle-specific proteins in cultured myoblasts and in the Rh30 cell line [4].

Biological context of PD 0332991

  • PD 0332991 is a highly specific inhibitor of cyclin-dependent kinase 4 (Cdk4) (IC50, 0.011 micromol/L) and Cdk6 (IC50, 0.016 micromol/L), having no activity against a panel of 36 additional protein kinases [5].

Analytical, diagnostic and therapeutic context of PD 0332991


  1. A novel orally active small molecule potently induces G1 arrest in primary myeloma cells and prevents tumor growth by specific inhibition of cyclin-dependent kinase 4/6. Baughn, L.B., Di Liberto, M., Wu, K., Toogood, P.L., Louie, T., Gottschalk, R., Niesvizky, R., Cho, H., Ely, S., Moore, M.A., Chen-Kiang, S. Cancer Res. (2006) [Pubmed]
  2. Phase I, Dose-Escalation Trial of the Oral Cyclin-Dependent Kinase 4/6 Inhibitor PD 0332991, Administered Using a 21-Day Schedule in Patients with Advanced Cancer. Flaherty, K.T., Lorusso, P.M., Demichele, A., Abramson, V.G., Courtney, R., Randolph, S.S., Shaik, M.N., Wilner, K.D., O'Dwyer, P.J., Schwartz, G.K. Clin. Cancer Res. (2012) [Pubmed]
  3. Palbociclib for the Treatment of Estrogen Receptor-Positive, HER2-Negative Metastatic Breast Cancer. Morikawa, A., Henry, N.L. Clin. Cancer Res. (2015) [Pubmed]
  4. Pharmacologic inhibition of cyclin-dependent kinase 4/6 activity arrests proliferation in myoblasts and rhabdomyosarcoma-derived cells. Saab, R., Bills, J.L., Miceli, A.P., Anderson, C.M., Khoury, J.D., Fry, D.W., Navid, F., Houghton, P.J., Skapek, S.X. Mol. Cancer Ther. (2006) [Pubmed]
  5. Specific inhibition of cyclin-dependent kinase 4/6 by PD 0332991 and associated antitumor activity in human tumor xenografts. Fry, D.W., Harvey, P.J., Keller, P.R., Elliott, W.L., Meade, M., Trachet, E., Albassam, M., Zheng, X., Leopold, W.R., Pryer, N.K., Toogood, P.L. Mol. Cancer Ther. (2004) [Pubmed]
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