Therapeutic Targets Database
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TTD Drug ID: DCL000152

Drug Information
NameLonafarnib
Synonyms1-Piperidinecarboxamide, 4-(2-(4-((11R)-3,10-dibromo-8-chloro-6,11-dihydro-5H-benzo(5,6)cyclohepta(1,2-b)pyridin-11-yl)-1-piperidinyl)-2-oxoethyl)-; D04768; ( )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; Lonafarnib (USAN/INN); SCH-066336; Sch-66336; CHEMBL298734; Sarasar; Lonafarnib [USAN]; 1o5m; AC1L3WMQ; 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)-; NSC719467; Sch 66336; CID148195; (+)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; AKOS005145760; (+)-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; Sch66336; C115354; LS-184039; Lonafarnib; 1-Piperidinecarboxamide, 4-(2-(4-((11R-3,10-dibromo-8-chloro-6,11-dihydro-5H-benzo(5,6)cyclohepta(1,2-b)pyridin-11-yl)-1-piperidinyl)-2-oxoethyl)-; UNII-IOW153004F; (+)-4-(2-(4-(11R)-3,10-Dibromo-8-chloro-6,11-dihydro-5H-benzo(5,6)cyclohepta(1,2-b)pyridin-11-yl)-piperidin-1-yl))-2-oxoethyl)-piperidine-1-carboxamide; 4-{2-[4-(3,10-DIBROMO-8-CHLORO-6,11-DIHYDRO-5H-BENZO[5,6]CYCLOHEPTA[1,2-B]PYRIDIN-11-YL)PIPERIDIN-1-YL]-2-OXOETHYL}PIPERIDINE-1-CARBOXAMIDE; 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; 193275-84-2
CompanySchering-Plough
IndicationNon-small cell lung cancer
[ICD9: 162   ICD10: C33, C34]
Terminated in Phase III    [1]
Structure

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InChI1S/C27H31Br2ClN4O2/c28-20-12-19-2-1-18-13-21(30)14-22(29)24(18)25
(26(19)32-15-20)17-5-9-33(10-6-17)23(35)11-16-3-7-34(8-4-16)27(31
)36/h12-17,25H,1-11H2,(H2,31,36)/t25-/m1/s1
InChIKeyDHMTURDWPRKSOA-RUZDIDTESA-N
Canonical SMILESC1CN(CCC1CC(=O)N2CCC(CC2)C3C4=C(C=C(C=C4CCC5=CC(=CN=C35)Br)Cl)Br)C(=O)N    
Isomeric SMILESC1CN(CCC1CC(=O)N2CCC(CC2)[C@@H]3C4=C(C=C(C=C4CCC5=CC(=CN=C35)Br)Cl)Br)C
(=O)N
Therapeutic ClassAntineoplastic Agents
CAS NumberCAS 193275-84-2
PubChem Compound IDCID 148195.
PubChem Substance IDSID 535096.
ClinicalTrials.govNCT00050336;
TargetFarnesyl protein transferaseInhibitor[2][3][4]
Ref 1Emerging therapies for multiple myeloma. Expert Opin Emerg Drugs. 2009 Mar;14(1):99-127. To Reference
Ref 2The protein farnesyltransferase regulates HDAC6 activity in a microtubule-dependent manner. J Biol Chem. 2009 Apr 10;284(15):9648-55. Epub 2009 Feb 18. To Reference
Ref 3Combining the farnesyltransferase inhibitor lonafarnib with paclitaxel results in enhanced growth inhibitory effects on human ovarian cancer models in vitro and in vivo. Gynecol Oncol. 2008 Apr;109(1):97-106. Epub 2008 Jan 31. To Reference
Ref 4A phase I safety, pharmacological, and biological study of the farnesyl protein transferase inhibitor, lonafarnib (SCH 663366), in combination with cisplatin and gemcitabine in patients with advanced solid tumors. Cancer Chemother Pharmacol. 2008 Sep;62(4):631-46. Epub 2007 Dec 6. To Reference



 

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