Drug Information

Drug (ID: DG01475) and It's Reported Resistant Information

• Name: Lonafarnib
• Synonyms: Lonafarnib; 193275-84-2; Sarasar; Sch66336; Sch 66336; Sch-66336; UNII-IOW153004F; CHEMBL298734; IOW153004F; (R)-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; 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]-; 4-[2-[4-(6,15-Dibromo-13-chloro-4-azatricyclo[9.4.0.03,8]pentadeca-1(11),3(8),4,6,12,14-hexaen-2-yl)piperidin-1-yl]-2-oxoethyl]piperidine-1-carboxamide; 4-[2-[4-[(2R)-6,15-dibromo-13-chloro-4-azatricyclo[9.4.0.03,8]pentadeca-1(11),3(8),4,6,12,14-hexaen-2-yl]piperidin-1-yl]-2-oxoethyl]piperidine-1-carboxamide; Zokinvy; 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)-; 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; SMR004701448; Lonafarnib (USAN/INN); Lonafarnib [USAN:INN]; C27H31Br2ClN4O2; Lonafarnib (SCH66336); lonafarnibum; 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-066336; 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]-1-piperidinecarboxamide; 1o5m; (non-labelled)Lonafarnib-d9; SCHEMBL19032; Sarasar; ; ; SCH 66336; (+)-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; MLS006010423; MLS006011106; GTPL8024; Lonafarnib, >=98% (HPLC); BDBM14459; CHEBI:47097; DTXSID90172927; BCP07027; EX-A1630; ZINC3950115; NSC719467; s2797; AKOS005145760; CCG-270312; CS-0792; DB06448; NSC-719467; NCGC00346707-01; 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)-; AC-32661; AS-56182; HY-15136; SW220034-1; Y0240; C73675; D04768; J-514232; Q3258910; (+)-4-[2-[4-(8-Chloro-3,10-dibromo-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11(R)-yl)-1-piperidin-yl]-2-oxo-ethyl]-1-piperidinecarboxamide; (+)-4[2-[4-(8-Chloro-3,11-dihydro-5H-benzo[5,6] cyclohepta[1,2-b]-pyridin-11(R)-yl-1-piperidinyl]-2-oxo-ethyl]-1-piperidinecarboxamide; 4-(2-{4-[(2R)-6,15-dibromo-13-chloro-4-azatricyclo[9.4.0.0^{3,8}]pentadeca-1(11),3,5,7,12,14-hexaen-2-yl]piperidin-1-yl}-2-oxoethyl)piperidine-1-carboxamide; 4-[2-[4-[(11R)-3,10-dibromo-8-chloro-6,11-dihydro-5H-benzo[1,2]cyclohepta[2,4-b]pyridin-11-yl]piperidin-1-yl]-2-oxoethyl]piperidine-1-carboxamide; 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]-1-Piperidi necarboxamide
• Indication:
  In total 1 Indication(s)
  Human immunodeficiency virus infection [ICD-11: 1C60-1C62]; Approved; [1]
• Drug Resistance Disease(s):
  Disease(s) with Clinically Reported Resistance for This Drug (1 diseases)
  Ovarian cancer [ICD-11: 2C73]; [1]
• Target: Human immunodeficiency virus Protease (HIV PR); POL_HV1B1; [1]
• Formula: 3
• IsoSMILES: C1CN(CCC1CC(=O)N2CCC(CC2)[C@@H]3C4=C(CCC5=C3N=CC(=C5)Br)C=C(C=C4Br)Cl)C(=O)N
• InChI: InChI=1S/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
• InChIKey: DHMTURDWPRKSOA-RUZDIDTESA-N
• PubChem CID: 148195
• ChEBI ID: CHEBI:47097
• TTD Drug ID: D07IQS
• VARIDT ID: DR1861
• DrugBank ID: DB06448

Type(s) of Resistant Mechanism of This Drug

  ADTT: Aberration of the Drug's Therapeutic Target

Drug Resistance Data Categorized by Their Corresponding Diseases

ICD-02: Benign/in-situ/malignant neoplasm

Ovarian cancer [ICD-11: 2C73]

Drug Resistance Data Categorized by Their Corresponding Mechanisms

Aberration of the Drug's Therapeutic Target (ADTT)

Key Molecule: Protein farnesyltransferase subunit beta (FNTB) [1]

• Molecule Alteration: Noncoding; (c.7-17904G>C)
• Resistant Disease: Ovarian cancer [ICD-11: 2C73.0]
• Experimental Note: Identified from the Human Clinical Data
• In Vitro Model: Ovary; N.A.
• Experiment for Molecule Alteration: Western blotting analysis
• Experiment for Drug Resistance: electrophoretic-mobility-shift assay; luciferase-reporter assay; RT-qPCR

References

• Ref 1: The FNTB promoter polymorphism rs11623866 as a potential predictive biomarker for lonafarnib treatment of ovarian cancer patientsBr J Clin Pharmacol. 2015 Nov;80(5):1139-48. doi: 10.1111/bcp.12688. Epub 2015 Jul 22.