lonafarnib (SCH 66336)

inhibitor of farnesyl protein transferase

Also Known As:

SCH 66336; (+)4-(2-(4-(8-chloro-3,10-dibromo-6,11-dihydro-5H-benzo(5,6)cyclohepta(1,2-b)pyridin-11-yl)-1-piperidinyl)-2-oxoethyl)-1-piperidinecarboxamide; 1-piperidinecarboxamide, 4(2-(4-(11R-3,10-dibromo-8-chloro-6,11-dihydro-5H-benzo(5,6)cyclohepta(1,2-b)pyridine-11-yl)-1-piperidinyl)-2-oxoethyl)-; 4-(2-(4-(8-chloro-3,10-dibromo-6,11-dihydro-5H-benzo-(5,6)-cyclohepta(1,2-b)-pyridin-11(R)-yl)-1-piperidinyl)-2-oxo-ethyl)-1-piperidinecarboxamide; SCH-66336; SCH66336; Sarasar; Zokinvy

Networked: 142 relevant articles (16 outcomes, 54 trials/studies)

Relationship Network

Bio-Agent Context: Research Results

Experts

1.	Khuri, Fadlo R: 9 articles (09/2011 - 05/2004)
2.	Kirschmeier, Paul: 8 articles (12/2009 - 08/2002)
3.	Lee, Ho-Young: 7 articles (08/2012 - 08/2003)
4.	Statkevich, Paul: 7 articles (11/2011 - 05/2004)
5.	Kieran, Mark W: 6 articles (01/2018 - 07/2007)
6.	Zhu, Yali: 6 articles (11/2011 - 05/2004)
7.	Bishop, W Robert: 6 articles (12/2009 - 01/2003)
8.	Kim, Edward S: 5 articles (08/2012 - 05/2004)
9.	Kirschmeier, P: 5 articles (09/2008 - 04/2000)
10.	Bishop, W R: 5 articles (03/2001 - 01/2000)

Related Diseases

1.	Neoplasms (Cancer) 12/01/1999 - "Greater combined efficacy for SCH66336 and SCH58500 was also observed in vivo in the DU-145 human prostate and wap-ras/F transgenic mouse cancer models." 10/01/2007 - "Additionally, a multiple-dose study was performed in 19 patients with advanced cancer who received lonafarnib 200 mg Q 12 H for 28 days under fasted and fed conditions. " 04/01/2007 - "Importantly, apparently similar chromosomal alignment defects were observed in head and neck tumors samples from a phase I trial with lonafarnib, providing support that lonafarnib disrupts chromosomal maintenance in human cancers. " 09/02/2005 - "These studies demonstrated that Rheb is modified by farnesylation, is not a substrate for alternative prenylation, and plays a role in SCH66336 enhancement of the anti-tumor response to other chemotherapeutics." 01/02/2003 - "SCH 66336 is a trihalo tricyclic compound that is currently undergoing Phase II clinical trials for the treatment of solid tumors. "
2.	Bone Diseases (Bone Disease) 07/12/2016 - "A previous single-arm clinical trial demonstrated that the protein farnesyltransferase inhibitor lonafarnib ameliorates some aspects of cardiovascular and bone disease. " 01/01/2018 - "The protein farnesyltransferase inhibitor, lonafarnib, ameliorates some aspects of cardiovascular and bone disease.MethodsWe performed a prospective longitudinal survey of plasma proteins in 24 children with HGPS (an estimated 10% of the world's population at the time) at baseline and on lonafarnib therapy, compared with age- and gender-matched controls using a multi-analyte, microsphere-based immunofluorescent assay.ResultsThe mean levels for 23/66 (34.8%) proteins were significantly lower and 7/66 (10.6%) were significantly higher in HGPS samples compared with those in controls (P≤0.05). "
3.	Non-Small-Cell Lung Carcinoma (Carcinoma, Non-Small Cell Lung) 11/01/2004 - "This study investigated whether Lonafarnib was effective in inhibiting the growth of human nonsmall cell lung cancer (NSCLC) cells and elucidated the role of Akt in mediating such growth inhibitory effects. " 05/01/2004 - "Additional studies of lonafarnib in combination regimens appear warranted, particularly in patients with non-small cell lung cancer." 03/01/2008 - "The FTI SCH66336 has been shown to induce apoptotic and antiangiogenic activities in a subset of head and neck squamous cell carcinoma (HNSCC) and non-small cell lung cancer (NSCLC) cell lines. " 02/01/2004 - "In vitro study of farnesyltransferase inhibitor SCH 66336, in combination with chemotherapy and radiation, in non-small cell lung cancer cell lines." 04/01/1999 - "The broad spectrum of soft agar growth inhibition by SCH 66336 in the human tumor cloning assay, and its efficacy at physiologically relevant concentrations in animal models, suggest that SCH 66336 may deserve future clinical trials in patients with ovarian, breast and non-small-cell lung cancer."
4.	Breast Neoplasms (Breast Cancer) 04/01/2023 - "Structure-activity relationship study to improve cytotoxicity and selectivity of lonafarnib against breast cancer cells." 04/01/2023 - "Therefore, we structurally modified the terminal 4-methylpiperidine-1-carboxamide residue of lonafarnib and evaluated the antiproliferative effects of the resulting derivatives in Michigan Cancer Foundation - 7 (MCF-7) breast cancer cells as well as simian virus 80 (SV-80) fibroblasts. " 09/01/2007 - "These studies indicate that lonafarnib enhances the efficacy of endocrine agents clinically used for treating hormone-dependent breast cancer." 09/01/2007 - "In four of five human breast cancer cell lines, lonafarnib enhanced the antiproliferative effects of 4-hydroxy tamoxifen. " 01/01/2013 - "Promising preliminary antitumor activity warrants further evaluation of lonafarnib in combination with paclitaxel and trastuzumab in Her2-positive breast cancer."
5.	Ovarian Neoplasms (Ovarian Cancer) 11/01/2015 - "A multicentre AGO-OVAR-15 phase II trial reported an unfavourable effect of lonafarnib on the outcome of patients with advanced ovarian cancer. " 11/01/2015 - "The FNTB promoter polymorphism rs11623866 as a potential predictive biomarker for lonafarnib treatment of ovarian cancer patients." 04/01/2008 - "Lonafarnib enhances the antiproliferative effects of paclitaxel on ovarian cancer cells in vitro and ovarian tumor xenografts in vivo. " 08/01/2012 - "This study evaluates whether a molecular targeted therapy with the farnesyltransferase inhibitor lonafarnib added to standard chemotherapy in first-line treatment of advanced ovarian cancer (OC) could improve progression-free (PFS) and overall survival (OS). " 04/01/2008 - "Combining the farnesyltransferase inhibitor lonafarnib with paclitaxel results in enhanced growth inhibitory effects on human ovarian cancer models in vitro and in vivo."

Related Drugs and Biologics

1.	Farnesyltranstransferase (Farnesyltransferase)
2.	lonafarnib (SCH 66336)
3.	Paclitaxel (Taxol)
4.	p21(ras) farnesyl-protein transferase (protein farnesyltransferase)
5.	Transferases
6.	Proteins (Proteins, Gene)
7.	tipifarnib (R115777)
8.	Hormones (Hormone)
9.	taxane
10.	Carboplatin (JM8)

Related Therapies and Procedures

1.	Therapeutics
2.	Drug Therapy (Chemotherapy)
3.	Molecular Targeted Therapy
4.	Microspheres (Microsphere)
5.	Oral Administration