Drug Information

Drug (ID: DG02016) and It's Reported Resistant Information

• Name: Pitavastatin
• Synonyms: Pitavastatin; Itavastatin; Livalo; NK 104; Pitavastatin [INN]; Pitavastatin calcium; UNII-M5681Q5F9P; NK-104; C25H24FNO4; M5681Q5F9P; Zypitamag; Flovas; (3R,5S,6E)-7-(2-Cyclopropyl-4-(4-fluorophenyl)quinolin-3-yl)-3,5-dihydroxyhept-6-enoic acid; P 872441; P-872441; (3R,5S,6E)-7-[2-cyclopropyl-4-(4-fluorophenyl)quinolin-3-yl]-3,5-dihydroxyhept-6-enoic acid; ( )-(3R,5S,6E)-7-(2-Cyclopropyl-4-(4-fluorophenyl)-3-quinolyl)-3,5-dihydroxy-6-heptenoic acid; NK 104 (acid); Pitavastatin calcium (JAN)
• Indication:
  In total 1 Indication(s)
  . .; .
• Formula: C25H24FNO4
• IsoSMILES: C1CC1C2=NC3=CC=CC=C3C(=C2C=CC(CC(CC(=O)O)O)O)C4=CC=C(C=C4)F
• InChI: InChI=1S/C25H24FNO4/c26-17-9-7-15(8-10-17)24-20-3-1-2-4-22(20)27-25(16-5-6-16)21(24)12-11-18(28)13-19(29)14-23(30)31/h1-4,7-12,16,18-19,28-29H,5-6,13-14H2,(H,30,31)/b12-11+/t18-,19-/m1/s1
• InChIKey: VGYFMXBACGZSIL-MCBHFWOFSA-N
• PubChem CID: 5282452
• ChEBI ID: CHEBI:32020
• VARIDT ID: DR01545

Type(s) of Resistant Mechanism of This Drug

  MRAP: Metabolic Reprogramming via Altered Pathways

Drug Resistance Data Categorized by Their Corresponding Diseases

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

Lung cancer [ICD-11: 2C25]

Drug Sensitivity Data Categorized by Their Corresponding Mechanisms

Metabolic Reprogramming via Altered Pathways (MRAP)

Key Molecule: Epidermal growth factor receptor (EGFR) [1]

• Metabolic Type: Lipid metabolism
• Sensitive Disease: Lung adenocarcinoma [ICD-11: 2C25.0]
• Molecule Alteration: Mutation; .
• Experimental Note: Revealed Based on the Cell Line Data
• Cell Pathway Regulation: Hippo signaling pathway; Activation; hsa04390
• Cell Pathway Regulation: Insulin signaling pathway; Activation; hsa04910
• In Vivo Model: Female BALB/c-nu mice, with PC9 and PC9GR cells; Mice
• Experiment for Drug Resistance: Tumor volume assay
• Mechanism Description: PC9 gefitinib resistant strains were induced by low-dose maintenance. Cell culture and animal-related studies validated that the application of pitavastatin inhibited the proliferation of lung cancer cells, promoted cell apoptosis, and restrained the acquired resistance to EGFR-TKIs. KEGG pathway analysis showed that the hippo/YAP signaling pathway was activated in PC9GR cells relative to PC12 cells, and the YAP expression was inhibited by pitavastatin administration.

Key Molecule: Epidermal growth factor receptor (EGFR) [1]

• Metabolic Type: Lipid metabolism
• Sensitive Disease: Lung adenocarcinoma [ICD-11: 2C25.0]
• Molecule Alteration: Mutation; .
• Experimental Note: Revealed Based on the Cell Line Data
• Cell Pathway Regulation: Hippo signaling pathway; Activation; hsa04390
• Cell Pathway Regulation: Insulin signaling pathway; Activation; hsa04910
• In Vitro Model: NSCLC cells; Lung; Homo sapiens (Human); N.A.
• Experiment for Drug Resistance: Apoptosis rate assay
• Mechanism Description: PC9 gefitinib resistant strains were induced by low-dose maintenance. Cell culture and animal-related studies validated that the application of pitavastatin inhibited the proliferation of lung cancer cells, promoted cell apoptosis, and restrained the acquired resistance to EGFR-TKIs. KEGG pathway analysis showed that the hippo/YAP signaling pathway was activated in PC9GR cells relative to PC10 cells, and the YAP expression was inhibited by pitavastatin administration.

References

• Ref 1: Pitavastatin sensitizes the EGFR-TKI associated resistance in lung cancer by inhibiting YAP/AKT/BAD-BCL-2 pathway. Cancer Cell Int. 2024 Jun 28;24(1):224.