tipifarnib (R115777)

01/01/2006 - "R115777 is a promising treatment for breast cancer but the relation between effect and growth factor receptor and ras status has to be established."
01/01/2004 - "Clinical efficacy against breast cancer was seen for the FTI tipifarnib in a phase II study. "
03/01/2003 - "In terms of their potential use in the chemotherapeutic treatment of advanced breast cancer, a Phase II trial of R115777 (using either continuous or intermittent twice-daily oral dosing) has demonstrated promising activity (approximately 10% partial response rate). "
04/15/2009 - "Tipifarnib inhibits FTase activity in human breast tumors in vivo, is associated with down-regulation of p-STAT3, and enhances the breast pCR rate, thus meriting further evaluation."
06/01/2004 - "Preclinical evidence suggests that FTIs can inhibit breast cancers in vitro and in vivo, and a phase II trial of the FTI, R115777, in patients with advanced breast cancer produced encouraging results. "

04/01/2006 - "Thus, R115777 was active in the prevention and therapy of these chemically induced mammary cancers, but was strikingly more effective in cancers with HaRas mutations."
05/01/2003 - "Thus, 100 mg/kg R115777 was similarly effective in preventing lung tumors when administered during the promotional phase of carcinogenesis [that is, either 4 or 14 weeks after B(a)P], whereas the lower dose of 50 mg/kg R115777 was ineffective. "
04/01/2006 - "Both of these studies implied a high sensitivity of tumors with HaRas mutations to the effects of R115777. "
04/01/2006 - "In the therapeutic study, a surgical biopsy of a mammary cancer was done to determine HaRas status, and growth of the cancer was then followed during treatment of the rat with R115777. "
03/01/2006 - "Phase II and III trials of tipifarnib as monotherapy for breast, colorectal, lung (both non-small cell and small cell), brain, pancreatic and urothelial cancers have all been disappointing. "

05/15/2008 - "Phase II trial of tipifarnib as maintenance therapy in first complete remission in adults with acute myelogenous leukemia and poor-risk features."
01/01/2014 - "In the present study, we examined the action of tipifarnib in human acute myelogenous leukemia cell lines and clinical samples. "
10/01/2011 - "We report the results of a phase 1 dose-escalation study of tipifarnib, an oral FT inhibitor, in patients with relapsed, refractory or newly diagnosed (if over age 70) acute myelogenous leukemia (AML), on a week-on, week-off schedule. "
04/01/2009 - "Patients aged 60 years and over with previously untreated acute myeloid leukemia were enrolled in a Phase I study combining tipifarnib with standard induction therapy. "
04/01/2009 - "A phase I study of tipifarnib combined with conventional induction and consolidation therapy for previously untreated patients with acute myeloid leukemia aged 60 years and over."

03/01/2006 - "US FDA approval for tipifarnib awaits results of subsequent Phase III trials of the agent in elderly acute leukemia."
07/01/2001 - "The safety, biologic activity, clinical response, and pharmacokinetics of R115777, a potent, orally active FTI, were recently investigated in a phase I dose-ranging study in patients with acute leukemias. "
06/01/2001 - "This study was a phase 1 trial of orally administered R115777 in 35 adults with poor-risk acute leukemias. "
02/01/2011 - "Oral tipifarnib is well tolerated in children with leukemia on a twice daily for 2 days schedule at 300 mg/m(2) /dose."
06/01/2010 - "Pediatric early T-cell precursor leukemia with NF1 deletion and high-sensitivity in vitro to tipifarnib."

11/01/2007 - "Phase 1 study of tipifarnib in combination with imatinib for patients with chronic myelogenous leukemia in chronic phase after imatinib failure."
10/01/2002 - "In 20 patients with MDS, two cycles of oral R115777 for 3 consecutive weeks followed by a 1-week rest produced an overall response rate of 30%, consistent with 29% reported in poor-prognosis acute leukemia or blast-phase chronic myelogenous leukemia (CML). "
03/01/2003 - "Efficacy of the farnesyl transferase inhibitor R115777 in chronic myeloid leukemia and other hematologic malignancies."
11/01/2001 - "A phase I trial of R115777 in refractory and relapsed acute leukemias induced responses in 8 (32%) of 25 patients with acute myelogenous leukemia (including two complete remissions) and in two of three with chronic myelogenous leukemia in blast crisis. "
07/01/2001 - "Patients with acute myelogenous leukemia (AML), acute lymphocytic leukemia (ALL), or chronic myelogenous leukemia (CML) in blast crisis received R115777 100 mg, 300 mg, 600 mg, 900 mg, or 1,200 mg twice daily for 21 days. "