Drug Information

Drug (ID: DG00902) and It's Reported Resistant Information

• Name: Penfluridol
• Synonyms: PENFLURIDOL; 26864-56-2; 1-(4,4-bis(4-fluorophenyl)butyl)-4-(4-chloro-3-(trifluoromethyl)phenyl)piperidin-4-ol; Semap; TLP-607; McN-JR-16,341; 1-[4,4-Bis(4-fluorophenyl)butyl]-4-[4-chloro-3-(trifluoromethyl)phenyl]-4-piperidinol; R-16341; 1-[4,4-bis(4-fluorophenyl)butyl]-4-[4-chloro-3-(trifluoromethyl)phenyl]piperidin-4-ol; UNII-25TLU22Q8H; R 16341; CHEMBL47050; 25TLU22Q8H; MFCD00866714; 4-Piperidinol, 1-(4,4-bis(4-fluorophenyl)butyl)-4-(4-chloro-3-(trifluoromethyl)phenyl)-; 4-Piperidinol, 1-[4,4-bis(4-fluorophenyl)butyl]-4-[4-chloro-3-(trifluoromethyl)phenyl]-; NSC-759179; NCGC00165865-01; DSSTox_CID_28947; DSSTox_RID_83212; DSSTox_GSID_49021; C28H27ClF5NO; R 16,341; Penfluridolum; Penfluridolum [INN-Latin]; CAS-26864-56-2; EINECS 248-074-5; BRN 1558826; Micefal; Penfluridol [USAN:INN:BAN]; Semap (TN); Penfluridol (USAN/INN); R16341; SCHEMBL93939; 1-(4,4-Bis(p-fluorophenyl)butyl)-4-(4-chloro-alpha,alpha,alpha-trifluoro-m-tolyl)-4-piperidinol; 5-21-02-00409 (Beilstein Handbook Reference); MLS004774011; DTXSID5049021; CHEBI:92278; AOB5341; MCN-JR-16341; HMS3264L13; HMS3652G22; Pharmakon1600-01505691; ACT03196; BCP03695; HY-B1077; ZINC4217252; Tox21_113546; BDBM50026066; NSC759179; PDSP1_000470; PDSP2_000468; AKOS005065828; Tox21_113546_1; BCP9000014; CCG-269878; CS-4633; DB13791; KS-5104; NSC 759179; Penfluridol, >=97% (HPLC), powder; 1-[4,4-Bis(4-fluorophenyl)butyl]-4-[4-chloro-3(trifluoromethyl)phenyl]-4-piperidinol; 4-Piperidinol,1-[4,4-bis(4-fluorophenyl)butyl]-4-[4-chloro-3-(trifluoromethyl)phenyl]-; NCGC00165865-02; NCGC00165865-03; 4-Piperidinol, 1-(4,4-bis(p-fluorophenyl)butyl)-4-(4-chloro-alpha,alpha,alpha-trifluoro-m-tolyl)-; 4-Piperidinol, 4-(4-chloro-alpha,alpha,alpha-trifluoro-m-tolyl)-1-(4,4-bis(p-fluorophenyl)butyl)-; AC-15413; SMR003500704; BCP0726000159; SBI-0206898.P001; DB-017683; FT-0645031; P2076; S4151; SW219540-1; D02630; AB01566919_01; 864P562; A818637; L001145; SR-05000001779; Q2149707; SR-05000001779-1; W-107147; BRD-K15409150-001-01-7; 1-[4,4-bis(4-fluorophenyl)butyl]-4-[4-chloranyl-3-(trifluoromethyl)phenyl]piperidin-4-ol; 1-[4,4-bis(4-fluorophenyl)butyl]-4-[4-chloro-3-(trifluoromethyl)phenyl]-piperidin-4-ol; 1-[4,4-Bis-(4-fluoro-phenyl)-butyl]-4-(4-chloro-3-trifluoromethyl-phenyl)-piperidin-4-ol; 1-[4,4-Bis(p-fluorophenyl)butyl]-4-(4-chloro-.alpha.,.alpha.,.alpha.-trifluoro-m-tolyl)-4-piperidinol; 1-[4,4-Bis(p-flurophenyl)butyl]-4-(4-chloro-.alpha.,.alpha.,.alpha.-trifluoro-m-tolyl)-4-piperidinol; 4-Piperidinol, 4-(4-chloro-.alpha.,.alpha.,.alpha.-trifluoro-m-tolyl)-1-(4,4-bis(p-fluorophenyl)butyl)-; PENFLURIDOL1-[4,4-Bis-(4-fluoro-phenyl)-butyl]-4-(4-chloro-3-trifluoromethyl-phenyl)-piperidin-4-ol
• Indication:
  In total 1 Indication(s)
  Schizophrenia [ICD-11: 6A20]; Approved; [1]
• Target: Voltage-gated calcium channel alpha Cav3.1 (CACNA1G); CAC1G_HUMAN; [1]
• Formula: C28H27ClF5NO
• IsoSMILES: C1CN(CCC1(C2=CC(=C(C=C2)Cl)C(F)(F)F)O)CCCC(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F
• InChI: 1S/C28H27ClF5NO/c29-26-12-7-21(18-25(26)28(32,33)34)27(36)13-16-35(17-14-27)15-1-2-24(19-3-8-22(30)9-4-19)20-5-10-23(31)11-6-20/h3-12,18,24,36H,1-2,13-17H2
• InChIKey: MDLAAYDRRZXJIF-UHFFFAOYSA-N
• PubChem CID: 33630
• ChEBI ID: CHEBI:92278
• TTD Drug ID: D0CQ0Z

Type(s) of Resistant Mechanism of This Drug

  UAPP: Unusual Activation of Pro-survival Pathway

Drug Resistance Data Categorized by Their Corresponding Diseases

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

Pancreatic cancer [ICD-11: 2C10]

Drug Sensitivity Data Categorized by Their Corresponding Mechanisms

Unusual Activation of Pro-survival Pathway (UAPP)

Key Molecule: Autophagy-related protein LC3 B (MAP1LC3B) [1]

• Sensitive Disease: Pancreatic ductal adenocarcinoma [ICD-11: 2C10.0]
• Molecule Alteration: Expression; Up-regulation

Differential expression of the molecule in resistant disease

• Classification of Disease: Pancreatic cancer [ICD-11: 2C10]
• The Specified Disease: Pancreatic cancer
• The Studied Tissue: Pancreas
• The Expression Level of Disease Section Compare with the Healthy Individual Tissue: p-value: 4.86E-03; Fold-change: 9.00E-02; Z-score: 3.21E+00
• Experimental Note: Revealed Based on the Cell Line Data
• Cell Pathway Regulation: Cell apoptosis; Activation; hsa04210
• In Vitro Model: A549/Taxol cells; Lung; Homo sapiens (Human); CVCL_W218
• In Vitro Model: SW403 cells; Colon; Homo sapiens (Human); CVCL_0545
• In Vivo Model: Athymic nude mouse xenograft model; Mus musculus
• Experiment for Molecule Alteration: Western blot analysis
• Experiment for Drug Resistance: SRB assay
• Mechanism Description: One of the hallmarks of autophagy is the accumulation of LC3B and its localization in vesicular structures. We observed that penfluridol treatment enhanced the expression of LC3B and hence induced autophagy in pancreatic cancer cells.

References

• Ref 1: Penfluridol suppresses pancreatic tumor growth by autophagy-mediated apoptosis .Sci Rep. 2016 May 18;6:26165. doi: 10.1038/srep26165. 10.1038/srep26165