Targeted Inhibition of Farnesyltransferase in Locally Advanced Breast Cancer: A Phase I and II Trial of Tipifarnib Plus Dose-Dense Doxorubicin and Cyclophosphamide

Sparano, Joseph A.; Moulder, Stacy L.; Kazi, Aslamuzzaman; Vahdat, Linda T.; Li, Tianhong; Pellegrino, C.; Munster, P.N.; Malafa, Mokenge P.; Lee, David; Hoschander, S.; Hopkins, Una; Hershman, Dawn L.; Wright, John J.; Sebti, Saı̈d M.

doi:10.1200/jco.2005.04.9114

Cited by 63 publications

(48 citation statements)

References 22 publications

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“…27 So inhibiting the function from the [28][29] However, combinations of FTIs with other therapies still hold great promise for therapeutic advances against cancer.…”

Section: Discussionmentioning

confidence: 99%

Selectively oncolytic mutant of HSV-1 lyses HeLa cells mediated by Ras/RTN3

Zhu

Xiao

et al. 2007

Cancer Biology & Therapy

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“…27 So inhibiting the function from the [28][29] However, combinations of FTIs with other therapies still hold great promise for therapeutic advances against cancer.…”

Section: Discussionmentioning

confidence: 99%

Selectively oncolytic mutant of HSV-1 lyses HeLa cells mediated by Ras/RTN3

Zhu

Xiao

et al. 2007

Cancer Biology & Therapy

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“…The regimen was safe and clinically active. Pathologic complete response in the breast was seen in 7 of 21 (33%) patients, which is only slightly more active than the standard response observed for doxorubicin and cyclophosphamide (52).…”

Section: Agents That Act On Cytosolic Eventsmentioning

confidence: 99%

Identifying Breast Cancer Druggable Oncogenic Alterations: Lessons Learned and Future Targeted Options

Ocaña

Pandiella

2008

Clinical Cancer Research

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Although the introduction of novel therapies and drug combinations has improved the prognosis of metastatic breast cancer, this disease remains incurable. It is therefore important to develop additional novel therapeutic strategies and agents. Increased understanding of the biology and the molecular alterations present in breast cancer is facilitating the design of targeted therapies directed to oncogenic proteins. Here, we review the signaling pathways and proteins that participate in breast cancer proliferation and survival, with special emphasis in those that are druggable.We will also comment on how the knowledge on the basic pathogenetic processes is translated into drug development strategies that are reaching the breast cancer clinic.

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“…They concluded that Tipifarnib may be safely combined with dose-dense cyclophosphamide using a dose and schedule that significantly inhibits FTase enzyme activity in human breast cancer in vivo and may enhance the pathologic complete response rate after four cycles of pre-operative dosedense cyclophosphamide [106].…”

Section: Combination Theraphymentioning

confidence: 99%

Inhibition of farnesyltransferase: A rational approach to treat cancer?

Puntambekar

Giridhar

Yadav

2007

Journal of Enzyme Inhibition and Medicinal Chemistry

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This article presents in brief the development of farnesyltransferase inhibitors (FTIs) and their preclinical and clinical status. In this review the mechanism of action of FTIs is discussed and their selectivity issue towards tumor cells is also addressed. The significant efficacy of FTIs as single or combined agents in preclinical studies stands in contrast with only moderate effects in Clinical Phase II-III studies. This suggests that there is a need to further explore and understand the complex mechanism of action of FTIs and their interaction with cytotoxic agents.

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Targeted Inhibition of Farnesyltransferase in Locally Advanced Breast Cancer: A Phase I and II Trial of Tipifarnib Plus Dose-Dense Doxorubicin and Cyclophosphamide

Abstract: Tipifarnib may be safely combined with dose-dense AC using a dose and schedule that significantly inhibits FTase enzyme activity in human breast cancer in vivo and may enhance the pCR rate after four cycles of preoperative dose-dense AC.

Cited by 63 publications

References 22 publications

Selectively oncolytic mutant of HSV-1 lyses HeLa cells mediated by Ras/RTN3

Selectively oncolytic mutant of HSV-1 lyses HeLa cells mediated by Ras/RTN3

Identifying Breast Cancer Druggable Oncogenic Alterations: Lessons Learned and Future Targeted Options

Inhibition of farnesyltransferase: A rational approach to treat cancer?

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