General Information of Drug (ID: DM9OZWQ)

Drug Name
Lovastatin Drug Info
Synonyms
lovastatin; 75330-75-5; mevinolin; Mevacor; Lovalip; Monacolin K; Lovalord; Mevinacor; Altoprev; Nergadan; Artein; Altocor; 6alpha-Methylcompactin; MK-803; Hipovastin; Lovastatine; Lovasterol; Paschol; Lipivas; Closterol; Teroltrat; Tecnolip; Rovacor; Cholestra; Rodatin; Lozutin; Lipofren; Lestatin; Hipolip; Colevix; Sivlor; Taucor; Lipdip; Belvas; Mevlor; Lovastatine [French]; Lovastatinum [Latin]; Lovastatina [Spanish]; 6-alpha-Methylcompactin; Lovastatinum; Lovastatina; Lovastin; MSD 803; MK 803; 6 alpha-Methylcompactin; UNII-9LHU78OQFD; Altocor; Liposcler; Mevinolin; Rextat; Sivlor;Taucor; Monakolin K; MK803; Advicor (TN); Altocor (TN); Altoprev (TN); L-154803; Lovastatin & Primycin; ML-530B; Mevacor (TN); Mevinolin from Aspergillus sp; Statosan (TN); Lovastatin (USP/INN); Lovastatin [USAN:BAN:INN]; Lovastatin, (1 alpha(S*))-Isomer; Lovastatin, 1 alpha-Isomer (without R*/S* notation); 2beta,6alpha-Dimethyl-8alpha-(2-methyl-1-oxobutoxy)-mevinic acid lactone; 6 Methylcompactin; 6-Methylcompactin; Aspirin/lisinopril/ lovastatin fixed-dose combination
Indication
Disease Entry ICD 11 Status REF
Arteriosclerosis BD40 Approved [1]
Hypercholesterolaemia 5C80.0 Approved [2]
Hyperlipidemia 5C80.Z Approved [1]
Hyperlipidemia, familial combined, LPL related Approved [1]
Hypertriglyceridemia 5C80.1 Approved [1]
Melanoma 2C30 Approved [1]
X-linked chondrodysplasia punctata 2 Approved [1]
Cardiovascular disease BA00-BE2Z Phase 3 [3]
Smith-Lemli-Opitz syndrome Investigative [1]
Therapeutic Class
Anticholesteremic Agents
Cross-matching ID
PubChem CID
53232
ChEBI ID
CHEBI:40303
CAS Number
CAS 75330-75-5
TTD Drug ID
DM9OZWQ
VARIDT Drug ID
DR00410
INTEDE Drug ID
DR0986
ACDINA Drug ID
D00377

Molecule(s) Related to This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
HMG-CoA reductase (HMGCR) TTPADOQ HMDH_HUMAN Inhibitor [4]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID Highest Status REF
Organic anion transporting polypeptide 1B1 (SLCO1B1) DT3D8F0 SO1B1_HUMAN Approved [5]
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Approved [6]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID Highest Status REF
Cytochrome P450 3A4 (CYP3A4) DE4LYSA CP3A4_HUMAN Approved [7]
UDP-glucuronosyltransferase 1A1 (UGT1A1) DEYGVN4 UD11_HUMAN Approved [8]
Mephenytoin 4-hydroxylase (CYP2C19) DEGTFWK CP2CJ_HUMAN Approved [8]
Cytochrome P450 2C8 (CYP2C8) DES5XRU CP2C8_HUMAN Approved [8]
UDP-glucuronosyltransferase 2B7 (UGT2B7) DEB3CV1 UD2B7_HUMAN Approved [8]
UDP-glucuronosyltransferase 1A3 (UGT1A3) DEF2WXN UD13_HUMAN Approved [8]
Serum paraoxonase/lactonase 3 (PON3) DETXQZ1 PON3_HUMAN Approved [9]

The Expression Level of Molecule(s) in Normal Tissue of Major ADME-Related Organs

Molecule Molecule Type Gene Name Liver Colon Kidney Small Intestine
HMG-CoA reductase (HMGCR) DTT HMGCR 6.357 6.256 5.17 6.85
P-glycoprotein 1 (ABCB1) DTP P-GP 7.009 6.988 7.442 8.135
Organic anion transporting polypeptide 1B1 (SLCO1B1) DTP OATP1B1 9.79 0.485 3.511 2.07
Serum paraoxonase/lactonase 3 (PON3) DME PON3 11.187 6.211 7.033 6.75
Cytochrome P450 2C8 (CYP2C8) DME CYP2C8 9.791 3.744 3.413 1.609
Mephenytoin 4-hydroxylase (CYP2C19) DME CYP2C19 7.867 5.142 5.52 7.08
Cytochrome P450 3A4 (CYP3A4) DME CYP3A4 11.692 6.58 4.984 9.089
Molecule Expression Atlas in Normal Tissue of Major ADME-related organs

The Expression Level of Molecule(s) between Disease Section and Healthy Individual Tissue

The Studied Disease Arteriosclerosis
ICD Disease Classification BD40
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
HMG-CoA reductase (HMGCR) DTT HMGCR 1.01E-05 0.65 1.53
P-glycoprotein 1 (ABCB1) DTP P-GP 3.29E-14 -7.08E-01 -1.99E+00
Organic anion transporting polypeptide 1B1 (SLCO1B1) DTP OATP1B1 3.27E-01 -5.78E-02 -3.84E-01
UDP-glucuronosyltransferase 1A1 (UGT1A1) DME UGT1A1 2.00E-01 5.79E-02 3.00E-01
Serum paraoxonase/lactonase 3 (PON3) DME PON3 2.30E-02 -3.44E-01 -1.20E+00
Cytochrome P450 2C8 (CYP2C8) DME CYP2C8 1.47E-02 -1.13E-01 -1.13E+00
Mephenytoin 4-hydroxylase (CYP2C19) DME CYP2C19 4.03E-02 -1.19E-01 -5.11E-01
Cytochrome P450 3A4 (CYP3A4) DME CYP3A4 3.24E-05 -3.48E-01 -1.34E+00
Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

References

1 Lovastatin FDA Label
2 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 2739).
3 Clinical pipeline report, company report or official report of CardioPharma Wilmington.
4 Microarray and biochemical analysis of lovastatin-induced apoptosis of squamous cell carcinomas. Neoplasia. 2002 Jul-Aug;4(4):337-46.
5 A novel human hepatic organic anion transporting polypeptide (OATP2). Identification of a liver-specific human organic anion transporting polypeptide and identification of rat and human hydroxymethylglutaryl-CoA reductase inhibitor transporters. J Biol Chem. 1999 Dec 24;274(52):37161-8.
6 Mammalian drug efflux transporters of the ATP binding cassette (ABC) family in multidrug resistance: A review of the past decade. Cancer Lett. 2016 Jan 1;370(1):153-64.
7 Metabolic interactions with statins. Tidsskr Nor Laegeforen. 2001 Jan 20;121(2):189-93.
8 Pharmacogenomics of statins: understanding susceptibility to adverse effects. Pharmgenomics Pers Med. 2016 Oct 3;9:97-106.
9 Paraoxonases-1, -2 and -3: what are their functions? Chem Biol Interact. 2016 Nov 25;259(Pt B):51-62.