Detail

R115777

Description

Name: R115777
Type: small molecule
Groups: investigational
Indication: Investigated for use/treatment in colorectal cancer, leukemia (myeloid), pancreatic cancer, and solid tumors.
Accession Number: DB04960 ( DB04960)
Description: R115777 is a substance that is being studied in the treatment of acute myeloid leukemia (AML) and other types of cancer. It belongs to the family of drugs called farnesyltransferase inhibitors. It is also called tipifarnib and Zarnestra.
Structure:
Prescription Products: Not Available
Generic Prescription Products: Not Available
Over the Counter Products: Not Available
International Brands
  • No Brands

Brand Names
  • No Brands

Brand Mixtures
Brand NameIngredients

Categories
  • Antineoplastic Agents

Pharmacology

Indication: Investigated for use/treatment in colorectal cancer, leukemia (myeloid), pancreatic cancer, and solid tumors.
Pharmacodynamics: Not Available
Mechanism of action: The farnesyltransferase inhibitors (FTIs) are a class of experimental cancer drugs that target protein farnesyltransferase with the downstream effect of preventing the proper functioning of the Ras protein, which is commonly abnormally active in cancer. After translation, RAS goes through four steps of modification: isoprenylation, proteolysis, methylation and palmitoylation. Isoprenylation involves the enzyme farnesyltransferase (FTase) transferring a farnesyl group from farnesyl pyrophosphate (FPP) to the pre-RAS protein. Also, a related enzyme geranylgeranyltransferase I (GGTase I) has the ability to transfer a geranylgeranyl group to K and N-RAS. Farnesyl is necessary to attach RAS to the cell membrane. Without attachment to the cell membrane, RAS is not able to transfer signals from membrane receptors (Reuter et al., 2000).
Absorption: Not Available
Volume of distribution: Not Available
Protein binding: Not Available
Metabolism: Not Available
Route of elimination: Not Available
Half life: Not Available
Clearance: Not Available
Toxicity: Not Available
Affected organisms
  • Not Available

SNP Mediated Adverse Drug Reactions
  • Not Available

Pharmacoeconomics

Manufacturers:
  • Not Available

Packagers:
  • Not Available

Dosage forms
FormRouteStrength

Prices
Unit descriptionCostUnit

Patents
CountryPatent NumberApprovedExpires (estimated)

Interactions

Drug Interactions
DrugInteraction

Food Interactions:
  • Not Available

Taxonomy

Kingdom: Organic compounds
Super Class: Not Available
Class: Not Available
Sub Class: Not Available
Direct Parent: Not Available
Alternative Parents:
  • Aralkylamines
  • Aryl chlorides
  • Azacyclic compounds
  • Chlorobenzenes
  • Heteroaromatic compounds
  • Hydrocarbon derivatives
  • Hydroquinolines
  • Hydroquinolones
  • Lactams
  • Monoalkylamines
  • N-substituted imidazoles
  • Organochlorides
  • Organooxygen compounds
  • Phenylpyridines
  • Phenylquinolines
  • Pyridinones

substituent:
  • 4-phenylpyridine
  • Amine
  • Aralkylamine
  • Aromatic heteropolycyclic compound
  • Aryl chloride
  • Aryl halide
  • Azacycle
  • Azole
  • Benzenoid
  • Chlorobenzene
  • Dihydroquinoline
  • Dihydroquinolone
  • Halobenzene
  • Heteroaromatic compound
  • Hydrocarbon derivative
  • Imidazole
  • Lactam
  • Linear 1,7-diphenylheptane skeleton
  • Monocyclic benzene moiety
  • N-substituted imidazole
  • Organochloride
  • Organohalogen compound
  • Organoheterocyclic compound
  • Organonitrogen compound
  • Organooxygen compound
  • Phenylquinoline
  • Primary aliphatic amine
  • Primary amine
  • Pyridine
  • Pyridinone
  • Quinoline

References

Synthesis Reference: Not Available
General Reference: # Martin LA, Head JE, Pancholi S, Salter J, Quinn E, Detre S, Kaye S, Howes A, Dowsett M, Johnston SR: The farnesyltransferase inhibitor R115777 (tipifarnib) in combination with tamoxifen acts synergistically to inhibit MCF-7 breast cancer cell proliferation and cell cycle progression in vitro and in vivo. Mol Cancer Ther. 2007 Sep;6(9):2458-67. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/17876043 # Wang CC, Liao YP, Mischel PS, Iwamoto KS, Cacalano NA, McBride WH: HDJ-2 as a target for radiosensitization of glioblastoma multiforme cells by the farnesyltransferase inhibitor R115777 and the role of the p53/p21 pathway. Cancer Res. 2006 Jul 1;66(13):6756-62. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/16818651
External Links:
ResourceLink

ATC Codes:
  • Not Available

AHFS Codes:
  • Not Available

MSDS: Download
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