tipifarnib (R115777)

farnesyltranstransferase inhibitor

Also Known As:

R115777; Zarnestra; (R)-6-(amino(4-chlorophenyl)(1-methyl-1H-imidazol-5-yl)methyl)-4-(3-chlorophenyl)-1-methyl-2(1H)-quinolinone; 2 (1H))-quinolinone,6-(amino(4-chlorophenyl)(1-methyl-1H-imidazol-5-yl)methyl)-4-(3-chlorophenyl)-1-methyl-,(+)-; R 115777; R-115777

Networked: 238 relevant articles (30 outcomes, 113 trials/studies)

Relationship Network

Bio-Agent Context: Research Results

Heterocyclic Compounds: 198
- Fused-Ring Heterocyclic Compounds
  - 2-Ring Heterocyclic Compounds
    - Quinolines: 146
      - Quinolones: 2938
        tipifarnib: 238

Experts

1.	Wright, John J: 20 articles (05/2014 - 04/2003)
2.	De Porre, Peter: 11 articles (06/2013 - 07/2006)
3.	Kurzrock, Razelle: 11 articles (04/2011 - 07/2002)
4.	Karp, Judith E: 10 articles (01/2014 - 07/2002)
5.	Lancet, Jeffrey E: 10 articles (03/2011 - 07/2002)
6.	Kaufmann, Scott H: 9 articles (01/2019 - 05/2003)
7.	Kantarjian, Hagop: 7 articles (03/2011 - 10/2002)
8.	Harousseau, Jean-Luc: 7 articles (08/2009 - 03/2007)
9.	Zhang, Steven: 7 articles (08/2007 - 10/2003)
10.	Adjei, Alex A: 6 articles (01/2014 - 05/2003)

Related Diseases

1.	Neoplasms (Cancer) 04/01/2006 - "Both of these studies implied a high sensitivity of tumors with HaRas mutations to the effects of 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. " 03/01/2005 - "We conducted a National Cancer Institute-sponsored phase I trial to determine the feasibility of an intermittent dosing schedule of R115777 given orally twice daily on weeks 1 and 3 of a 28-day cycle in patients with malignant solid tumors. " 06/08/2004 - "R115777 has been evaluated in phase III clinical trials and shows indications for the treatment of blood and breast malignancies. " 07/17/2023 - "In conclusion, tipifarnib has anti-tumor and anti-inflammatory effects in a NASH-related HCC model and may be a promising new agent to treat this disease."
2.	Breast Neoplasms (Breast Cancer) 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). " 01/01/2018 - "Patients and Methods 30 postmenopausal women with metastatic breast cancer were treated on a 21-day cycle with tipifarnib 300 mg PO twice daily from days 1 through 14. " 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." 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. "
3.	Squamous Cell Carcinoma of Head and Neck 10/01/2021 - "We evaluated the efficacy of tipifarnib in patients with R/M mHRAS HNSCC. " 10/02/2023 - "Tipifarnib Potentiates the Antitumor Effects of PI3Kα Inhibition in PIK3CA- and HRAS-Dysregulated HNSCC via Convergent Inhibition of mTOR Activity." 01/01/2022 - "With the advent of clinical evaluation of the FTI tipifarnib for the treatment of HRAS-mutant HNSCC, we investigated the activity of tipifarnib and inhibitors of HRAS effector signaling in HRAS-mutant HNSCC cell lines. " 11/01/2021 - "Treatment of wild-type H-Ras HNSCC cell lines in vitro with tipifarnib reduced cell growth and increased levels of defarnesylated H-Ras in a dose-dependent manner. " 10/01/2021 - "Tipifarnib demonstrated encouraging efficacy in patients with R/M HNSCC with HRAS mutations for whom limited therapeutic options exist (NCT02383927)."
4.	Acute Myeloid Leukemia (Acute Myelogenous Leukemia) 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. " 03/01/2008 - "We analyzed gene expression profiles from the bone marrow of patients from a phase 2 study of the FTI tipifarnib in older adults with previously untreated acute myeloid leukemia (AML). " 04/01/2007 - "Identification of molecular predictors of response in a study of tipifarnib treatment in relapsed and refractory acute myelogenous leukemia." 03/01/2014 - "We report on 348 patients ≥ 70 years (median age 78 years) with acute myeloid leukemia (>50% with secondary AML) randomized to receive either 600 mg or 300 mg of tipifarnib orally twice daily on days 1-21 or days 1-7 and 15-21, repeated every 28 days (4 treatment regimens). "
5.	Leukemia 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. " 01/05/2017 - "Tipifarnib, approved by USFDA for the treatment of elderly acute leukemia is a Ras pathway inhibitor. " 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."

Related Drugs and Biologics

1.	Transferases
2.	tipifarnib (R115777)
3.	Farnesyltranstransferase (Farnesyltransferase)
4.	Bortezomib (Velcade)
5.	Gemcitabine
6.	lonafarnib (SCH 66336)
7.	Imatinib Mesylate (Gleevec)
8.	Tamoxifen
9.	Docetaxel (Taxotere)
10.	Estrogen Receptors

Related Therapies and Procedures

1.	Therapeutics
2.	Precision Medicine
3.	Immunotherapy
4.	Radiotherapy
5.	Stents