Lovastatin
drug drugOn this page
Also known as 6.alpha.-methylcompactinAltoprevC10AA02L-154803Lovastatin component of advicorLovastatinaLovastatineMevacorMevinacorMevinacor 10Mevinacor 40MevinolinMevlorMK-803Monacolin kNSC-758662Simvastatin impuritylovastatin-Sivlor
Summary
Lovastatin (CHEMBL503) is an approved small-molecule antineoplastic agent (ATC C10AA02) targeting NR1I2 and HMGCR; indicated across 34 conditions including cardiovascular disorder and coronary artery disorder.
At a glance
- Status: Approved (max clinical phase 4)
- Modality: Small molecule
- ATC class: C10AA02
- Targets: 2 (NR1I2, HMGCR)
- Indications: 34 conditions
- Clinical trials: 51
- Chemistry: 404.5 Da · C24H36O5
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL503 |
| Name | Lovastatin |
| Type | Small molecule |
| Max phase | 4 |
| FDA approved | yes |
| PubChem CID | 53232 |
| ChEBI | CHEBI:40303 |
| ATC | C10AA02 |
| Molecular formula | C24H36O5 |
| Molecular weight | 404.5 |
| InChIKey | PCZOHLXUXFIOCF-BXMDZJJMSA-N |
SMILES: CC[C@H](C)C(=O)O[C@H]1C[C@H](C=C2[C@H]1[C@H]([C@H](C=C2)C)CC[C@@H]3C[C@H](CC(=O)O3)O)C
IUPAC name: [(1S,3R,7S,8S,8aR)-8-[2-[(2R,4R)-4-hydroxy-6-oxooxan-2-yl]ethyl]-3,7-dimethyl-1,2,3,7,8,8a-hexahydronaphthalen-1-yl] (2S)-2-methylbutanoate
ChEBI definition: A fatty acid ester that is mevastatin carrying an additional methyl group on the carbobicyclic skeleton. It is used in as an anticholesteremic drug and has been found in fungal species such as Aspergillus terreus and Pleurotus ostreatus (oyster mushroom).
Pharmacological roles (ChEBI): antineoplastic agent, prodrug, anticholesteremic drug.
Other ChEBI roles (chemical / environmental): Aspergillus metabolite.
Also known as: 6.alpha.-methylcompactin, Altoprev, C10AA02, L-154803, Lovastatin, Lovastatin component of advicor, Lovastatina, Lovastatine, Mevacor, Mevinacor, Mevinacor 10, Mevinacor 40
Patent coverage: 24,516 distinct patent families (92,462 SureChEMBL compound mentions), from 1 matched compound structure(s). Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.
Targets
Targets
Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).
| Gene | Target | Action | pAffinity | Cancer dependency | UniProt |
|---|---|---|---|---|---|
| NR1I2 | Pregnane X receptor | Full agonist | 6 | 0.3% | O75469 |
| HMGCR | hydroxymethylglutaryl-CoA reductase | Competitive | 7.3 | 84.4% | P04035 |
Broader ChEMBL bioactivity targets: 40 (assay-derived). Sample: Tyrosyl-DNA phosphodiesterase 1, Microtubule-associated protein tau, Lysine-specific demethylase 4E, Nuclear receptor ROR-gamma, Survival motor neuron protein, Fructose-bisphosphate aldolase, Prelamin-A/C, 4’-phosphopantetheinyl transferase ffp, Ferritin light chain, Solute carrier organic anion transporter family member 1B1, Integrin alpha-L, 5-hydroxytryptamine receptor 2B, Protein deacetylase HDAC6, Histone deacetylase 2, Thyrotropin receptor, Thromboxane A2 receptor, Progesterone receptor, Intercellular adhesion molecule (ICAM-1), Integrin alpha-L/beta-2, Sodium-dependent noradrenaline transporter, Adenosine receptor A1.
Bioactivity
ChEMBL activities: 44 potent at pChembl ≥ 5 of 89 total. Top 100 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| HMGCR | 9.22 | Ki | 0.6 | nM | CHEMBL_ACT_2430364 |
| HMGCR | 8.7 | IC50 | 2 | nM | CHEMBL_ACT_2430365 |
| HMGCR | 8.66 | IC50 | 2.2 | nM | CHEMBL_ACT_18168813 |
| P51639 | 8.66 | IC50 | 2.2 | nM | CHEMBL_ACT_25041351 |
| P51639 | 8.66 | IC50 | 2.2 | nM | CHEMBL_ACT_29284798 |
| P51639 | 8.52 | IC50 | 3 | nM | CHEMBL_ACT_174222 |
| P51639 | 8.15 | IC50 | 7 | nM | CHEMBL_ACT_725201 |
| P51639 | 8.1 | IC50 | 8 | nM | CHEMBL_ACT_1081602 |
| P51639 | 8.1 | IC50 | 8 | nM | CHEMBL_ACT_513025 |
| P51639 | 8.1 | IC50 | 8 | nM | CHEMBL_ACT_969431 |
| P51639 | 7.96 | IC50 | 11 | nM | CHEMBL_ACT_572903 |
| HMGCR | 7.7 | IC50 | 20 | nM | CHEMBL_ACT_1103907 |
| HMGCR | 7.7 | IC50 | 20 | nM | CHEMBL_ACT_7753303 |
| P51639 | 7.57 | IC50 | 27 | nM | CHEMBL_ACT_124891 |
| Q01237 | 7.57 | IC50 | 27 | nM | CHEMBL_ACT_378179 |
| P51639 | 7.55 | IC50 | 28 | nM | CHEMBL_ACT_1301610 |
| HMGCR | 7.53 | IC50 | 29.5 | nM | CHEMBL_ACT_12718210 |
| HMGCR | 7.53 | IC50 | 29.5 | nM | CHEMBL_ACT_17700742 |
| HMGCR | 7.53 | IC50 | 29.5 | nM | CHEMBL_ACT_17773210 |
| P51639 | 7.5 | IC50 | 32 | nM | CHEMBL_ACT_124892 |
| P51639 | 7.5 | IC50 | 32 | nM | CHEMBL_ACT_378180 |
| HMGCR | 7.43 | IC50 | 37 | nM | CHEMBL_ACT_108166 |
| HMGCR | 7.41 | IC50 | 39 | nM | CHEMBL_ACT_378181 |
| HMGCR | 7.3 | IC50 | 50 | nM | CHEMBL_ACT_1081603 |
| HMGCR | 7.3 | IC50 | 50 | nM | CHEMBL_ACT_969433 |
| P51639 | 6.4 | IC50 | 400 | nM | CHEMBL_ACT_173175 |
| P51639 | 6.28 | IC50 | 530 | nM | CHEMBL_ACT_1044595 |
| P81908 | 5.96 | Ki | 1100 | nM | CHEMBL_ACT_12481281 |
| ITGB2 | 5.62 | IC50 | 2400 | nM | CHEMBL_ACT_20604678 |
| O42275 | 5.57 | Ki | 2700 | nM | CHEMBL_ACT_12481277 |
| ITGB2 | 5.42 | IC50 | 3780 | nM | CHEMBL_ACT_511845 |
| P81908 | 5.3 | Ki | 5012 | nM | CHEMBL_ACT_12481295 |
| LMNA | 5.25 | Potency | 5623 | nM | CHEMBL_ACT_3643963 |
| P51450 | 5.15 | Potency | 7080 | nM | CHEMBL_ACT_4762927 |
| SLC6A3 | 5.09 | Ki | 8028 | nM | CHEMBL_ACT_7753274 |
| SLC6A2 | 5.06 | IC50 | 8753 | nM | CHEMBL_ACT_7753209 |
| SLC6A2 | 5.06 | Ki | 8680 | nM | CHEMBL_ACT_7753210 |
| TACR2 | 5.03 | Ki | 9408 | nM | CHEMBL_ACT_7755466 |
| ABCB1 | 5 | IC50 | 10000 | nM | CHEMBL_ACT_11000938 |
| HIF1A | 5 | Potency | 10000 | nM | CHEMBL_ACT_4125688 |
| HIF1A | 5 | Potency | 10000 | nM | CHEMBL_ACT_4519897 |
| CYP3A4 | 5 | Potency | 10000 | nM | CHEMBL_ACT_4977773 |
| CYP3A4 | 5 | Potency | 10000 | nM | CHEMBL_ACT_5046801 |
| SLC6A3 | 5 | IC50 | 10100 | nM | CHEMBL_ACT_7753273 |
Target pathways
Aggregated over 2 target gene(s): NR1I2, HMGCR.
Top Reactome pathways
7 total, by targets touching each:
| Pathway | Targets | Genes |
|---|---|---|
| Cholesterol biosynthesis | 1 | HMGCR |
| PPARA activates gene expression | 1 | HMGCR |
| Activation of gene expression by SREBF (SREBP) | 1 | HMGCR |
| Nuclear Receptor transcription pathway | 1 | NR1I2 |
| SUMOylation of intracellular receptors | 1 | NR1I2 |
| EGR2 and SOX10-mediated initiation of Schwann cell myelination | 1 | HMGCR |
| Lanosterol biosynthesis | 1 | HMGCR |
Dominant GO biological processes
| GO term | Targets |
|---|---|
| steroid metabolic process | 2 |
| negative regulation of transcription by RNA polymerase II | 1 |
| regulation of DNA-templated transcription | 1 |
| xenobiotic metabolic process | 1 |
| signal transduction | 1 |
| gene expression | 1 |
| positive regulation of gene expression | 1 |
| cell differentiation | 1 |
| intracellular receptor signaling pathway | 1 |
| xenobiotic catabolic process | 1 |
| xenobiotic transport | 1 |
| negative regulation of DNA-templated transcription | 1 |
| positive regulation of DNA-templated transcription | 1 |
| positive regulation of transcription by RNA polymerase II | 1 |
| intestinal epithelial structure maintenance | 1 |
Indications & clinical
Indications
3 approved indications. FDA phase 4, plus an anticancer drug’s labelled cancer uses (which ChEMBL often logs at phase 3).
| Indication | Phase | MONDO | EFO |
|---|---|---|---|
| cardiovascular disorder | 4 | MONDO:0004995 | EFO:0000319 |
| coronary artery disorder | 4 | MONDO:0005010 | EFO:0001645 |
| atherosclerosis | 4 | MONDO:0005311 | EFO:0003914 |
25 diseases in clinical trials (phase 1–3, investigational — not approved indications). Highest ChEMBL trial phase per disease; a non-cancer approved use is occasionally logged at phase 3 here.
| Disease (in trials) | Phase | MONDO | EFO |
|---|---|---|---|
| intermittent vascular claudication | 3 | MONDO:0005295 | EFO:0003876 |
| myocardial ischemia | 3 | MONDO:0024644 | EFO:1001375 |
| heart disorder | 3 | MONDO:0005267 | EFO:0003777 |
| peripheral vascular disease | 3 | MONDO:0005294 | EFO:0003875 |
| chronic obstructive pulmonary disease | 2 | MONDO:0005002 | EFO:0000341 |
| HIV infectious disease | 2 | MONDO:0005109 | EFO:0000764 |
| rheumatoid arthritis | 2 | MONDO:0008383 | EFO:0000685 |
| melanoma | 2 | MONDO:0005105 | EFO:0000756 |
| internal carotid artery stenosis | 2 | MONDO:0005189 | EFO:0002615 |
| cerebral atherosclerosis | 2 | MONDO:0006694 | EFO:1000860 |
| learning disability | 2 | MONDO:0004681 | MONDO:0004681 |
| breast neoplasm | 2 | MONDO:0021100 | MONDO:0007254 |
| ovarian cancer | 2 | MONDO:0008170 | MONDO:0008170 |
| arteriovenous malformations of the brain | 2 | MONDO:0007154 | Orphanet:46724 |
| Parkinson disease | 2 | MONDO:0005180 | MONDO:0005180 |
| cerebrotendinous xanthomatosis | 2 | MONDO:0008948 | MONDO:0008948 |
| fragile X syndrome | 2 | MONDO:0010383 | MONDO:0010383 |
| Rett syndrome | 2 | MONDO:0010726 | MONDO:0010726 |
| neurofibromatosis type 1 | 2 | MONDO:0018975 | MONDO:0018975 |
| cerebrovascular disorder | 2 | MONDO:0011057 | EFO:0003763 |
| stroke disorder | 1 | MONDO:0005098 | EFO:0000712 |
| acute myeloid leukemia | 1 | MONDO:0018874 | EFO:0000222 |
| metabolic disease | 1 | MONDO:0005066 | EFO:0000589 |
| porokeratosis | 1 | MONDO:0006602 | EFO:1000757 |
| asthma | 1 | MONDO:0004979 | MONDO:0004979 |
6 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.
Clinical trials
Total trials: 51.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE2 | 22 |
| PHASE3 | 9 |
| PHASE1 | 6 |
| Not specified | 6 |
| PHASE4 | 4 |
| PHASE1/PHASE2 | 2 |
| PHASE2/PHASE3 | 1 |
| EARLY_PHASE1 | 1 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT00345657 | PHASE4 | COMPLETED | Efficacy Study of Extended-Release Niacin/Lovastatin Versus Usual Care |
| NCT01346670 | PHASE4 | COMPLETED | Lovastatin and Its ß-hydroxy Acid From Four 600 mg LipoCol Forte® Capsules Compared to That of One 20 mg Mevacor® Tablet in Healthy Subjects |
| NCT01527669 | PHASE4 | COMPLETED | The Pharmacokinetic Study of Red Yeast Rice Capsule Compared to Lovastatin Tablet in Healthy Subjects |
| NCT02642653 | PHASE4 | COMPLETED | Combining Lovastatin and a Parent-Implemented Language Intervention for Fragile X Syndrome |
| NCT00000463 | PHASE3 | COMPLETED | Post Coronary Artery Bypass Graft (CABG) Study |
| NCT00000512 | PHASE3 | COMPLETED | Familial Atherosclerosis Treatment Study |
| NCT00062556 | PHASE3 | COMPLETED | Effect of Niacin ER/Lovastatin on Peak Walking Time & Claudication Onset Time in Patients With Intermittent Claudication |
| NCT00071266 | PHASE3 | COMPLETED | The Dose Response of Niacin ER/Lovastatin on Peak Walking Time (PWT) in Patients With Intermittent Claudication - TROPIC |
| NCT00092846 | PHASE3 | COMPLETED | A 6-Month Consumer Behavior Study of a Self-Management System (0803-084)(COMPLETED) |
| NCT00116870 | PHASE2/PHASE3 | COMPLETED | MARS - Monitored Atherosclerosis Regression Study |
| NCT00132717 | PHASE3 | COMPLETED | A 12 Week Study of MK0653A in Patients Who Have Been Hospitalized for a Possible Heart Problem (0653A-808) |
| NCT00718796 | PHASE3 | COMPLETED | Naturopathic Treatment for the Prevention of Cardiovascular Disease |
| NCT03510715 | PHASE3 | COMPLETED | An Efficacy and Safety Study of Alirocumab in Children and Adolescents With Homozygous Familial Hypercholesterolemia |
| NCT03510884 | PHASE3 | COMPLETED | An Efficacy and Safety Study of Alirocumab in Children and Adolescents With Heterozygous Familial Hypercholesterolemia |
| NCT02964884 | PHASE2 | ACTIVE_NOT_RECRUITING | Interventions for Reading Disabilities in NF1 |
| NCT06636734 | PHASE2 | RECRUITING | Lovastatin and Pembrolizumab for the Treatment of Patients With Recurrent or Metastatic Head and Neck Cancer, LAPP Trial |
| NCT00000469 | PHASE2 | COMPLETED | Asymptomatic Carotid Artery Plaque Study (ACAPS) |
| NCT00000477 | PHASE2 | COMPLETED | Cholesterol Reduction in Seniors Program (CRISP) |
| NCT00004346 | PHASE2 | UNKNOWN | Phase II Study of Cholesterol- and Cholestanol-Free Diet, Lovastatin, and Chenodeoxycholic Acid for Cerebrotendinous Xanthomatosis |
| NCT00285857 | PHASE2 | TERMINATED | Phase 2 Study of Lovastatin as Breast Cancer Chemoprevention |
| NCT00302952 | PHASE2 | TERMINATED | Lovastatin for the Treatment of Mildly Active Rheumatoid Arthritis |
| NCT00462280 | PHASE2 | COMPLETED | Lovastatin in Treating Patients At High Risk of Melanoma |
| NCT00580970 | PHASE2 | COMPLETED | Study of Effectiveness of Lovastatin to Prevent Radiation-Induced Rectal Injury |
| NCT00583102 | PHASE1/PHASE2 | TERMINATED | Dose Escalation Phase I/II Study of Lovastatin With High-Dose Cytarabine for Refractory or Relapsed AML |
| NCT00585052 | PHASE2 | TERMINATED | A Phase II Study of Interaction of Lovastatin and Paclitaxel For Patients With Refractory or Relapsed Ovarian Cancer |
| NCT00689806 | PHASE1/PHASE2 | WITHDRAWN | Evaluation of Lovastatin in Severe Persistent Asthma |
| NCT00700921 | PHASE2 | COMPLETED | Lovastatin as a Potential Modulator of Apoptosis in Chronic Obstructive Pulmonary Disease (COPD) |
| NCT00721305 | PHASE2 | COMPLETED | Lovastatin: Immunomodulatory Value Evaluation |
| NCT00902668 | PHASE2 | TERMINATED | Lovastatin in Reducing Side Effects After Radiation Therapy in Women With Breast Cancer |
| NCT00963664 | PHASE2 | WITHDRAWN | Evaluation of Interferon-Lovastatin Therapy for Malignant Melanoma |
| NCT01110642 | PHASE2 | WITHDRAWN | Novel Treatment for Syndromic Ichthyoses |
| NCT02389868 | PHASE2 | COMPLETED | Effects of Lovastatin on Human Platelet Proteome |
| NCT02563860 | PHASE2 | COMPLETED | Pharmacological Treatment of Rett Syndrome With Statins |
| NCT02680379 | PHASE2 | COMPLETED | Combined Treatment of Minocycline and Lovastatin to Treat Individuals With Fragile X Syndrome |
| NCT03242499 | PHASE2 | UNKNOWN | Lovastatin as a Neuroprotective Treatment for Early Stage Parkinson’s Disease |
| NCT03504501 | PHASE2 | TERMINATED | Synaptic Plasticity and Cognitive Function in RASopathies |
| NCT03981601 | PHASE2 | UNKNOWN | Evaluation, the Histomorphometric Study of Nanocrystalline Hydroxyapatite (Nano Bone) Wif Lovastatin in the Preservation of the Tooth Socket |
| NCT04297033 | PHASE2 | UNKNOWN | Lovastatin for Treatment of Brain Arteriovenous Malformations |
| NCT00243880 | PHASE1 | COMPLETED | Neuroprotection With Statin Therapy for Acute Recovery Trial (Neu-START) |
| NCT00352599 | PHASE1 | COMPLETED | Trial to Evaluate the Safety of Lovastatin in Individuals With Neurofibromatosis Type I (NF1) |
| NCT00584012 | PHASE1 | TERMINATED | A Study of the Proper Dosage of Lovastatin and Docetaxel for Patients With Cancer |
| NCT01250535 | PHASE1 | COMPLETED | Human Cytochrome P450 4F Enzymes and Drug Interactions |
| NCT02603770 | PHASE1 | COMPLETED | Compare Pharmacokinetic(PK) Profiles of XZK vs Lovastatin in Healthy Male Volunteers |
| NCT04359823 | PHASE1 | COMPLETED | DSAP Treatment Comparison: 2% Lovastatin/ 2% Cholesterol vs 2% Lovastatin Alone |
| NCT02998151 | EARLY_PHASE1 | COMPLETED | Neurophysiological and Acute Pharmacological Studies in FXS Patients |
| NCT01361217 | Not specified | COMPLETED | The Effects of Multiple Dose Fluoxetine and Metabolites on CYP1A2, CYP2C19, CYP2D6 and CYP3A4 Activity |
| NCT01478828 | Not specified | TERMINATED | Pre-Prostatectomy Lovastatin on Prostate Cancer |
| NCT02518503 | Not specified | COMPLETED | High Potency Statins and the Risk of Diabetes |
| NCT02518516 | Not specified | COMPLETED | High Potency Statins and Acute Kidney Injury |
| NCT03826940 | Not specified | COMPLETED | From Molecules to Cognition: Inhibitory Mechanisms in ASD and NF1 |
| NCT06789497 | Not specified | COMPLETED | The GABAergic Inhibitory System in Drug Resistant Epilepsy |
Clinical evidence (CIViC)
No CIViC predictive evidence (expected for non-precision-medicine drugs).
Pharmacology
Pharmacogenomics
PharmGKB dosing guidelines (3) — CPIC / DPWG genotype-guided dosing for this drug (drug × pharmacogene):
| Guideline | Source | Gene(s) | Dosing | Recommendation |
|---|---|---|---|---|
| Annotation of CPIC Guideline for lovastatin and SLCO1B1 | CPIC | SLCO1B1 | yes | yes |
| Annotation of CPIC Guideline for atorvastatin, fluvastatin, lovastatin | CPIC | ABCG2 | ||
| Annotation of CPIC Guideline for atorvastatin, fluvastatin, lovastatin | CPIC | CYP3A4;CYP3A5;HMGCR |
PharmGKB also curates 12 clinical and 17 variant annotation(s) for this drug (gene-keyed; see PharmGKB).
Related molecules
Related molecules
Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.
286 molecules share ≥1 primary target. Top 100 by shared-target count:
| Molecule | Source | Status | Shared targets |
|---|---|---|---|
| ATORVASTATIN | ChEMBL + PubChem | Phase 4 (approved) | HMGCR, NR1I2 |
| PITAVASTATIN | ChEMBL + PubChem | Phase 4 (approved) | HMGCR, NR1I2 |
| ROSUVASTATIN | ChEMBL + PubChem | Phase 4 (approved) | HMGCR, NR1I2 |
| SIMVASTATIN | ChEMBL + PubChem | Phase 4 (approved) | HMGCR, NR1I2 |
| VORINOSTAT | ChEMBL + PubChem | Phase 4 (approved) | HMGCR, NR1I2 |
| BOSENTAN | ChEMBL + PubChem | Phase 4 (approved) | NR1I2 |
| CRIZOTINIB | ChEMBL + PubChem | Phase 4 (approved) | NR1I2 |
| DACOMITINIB | ChEMBL + PubChem | Phase 4 (approved) | NR1I2 |
| DESOXYCORTICOSTERONE PIVALATE | ChEMBL + PubChem | Phase 4 (approved) | NR1I2 |
| FULVESTRANT | ChEMBL + PubChem | Phase 4 (approved) | NR1I2 |
| GEFITINIB | ChEMBL + PubChem | Phase 4 (approved) | NR1I2 |
| PRAVASTATIN | ChEMBL + PubChem | Phase 4 (approved) | HMGCR |
| TADALAFIL | ChEMBL + PubChem | Phase 4 (approved) | NR1I2 |
| ABACAVIR | ChEMBL | Phase 4 (approved) | NR1I2 |
| ACENOCOUMAROL | ChEMBL | Phase 4 (approved) | NR1I2 |
| ACETAMINOPHEN | ChEMBL | Phase 4 (approved) | NR1I2 |
| ACITRETIN | ChEMBL | Phase 4 (approved) | NR1I2 |
| ADAPALENE | ChEMBL | Phase 4 (approved) | NR1I2 |
| ALECTINIB | ChEMBL | Phase 4 (approved) | NR1I2 |
| ALPIDEM | ChEMBL | Phase 4 (approved) | NR1I2 |
| AMBRISENTAN | ChEMBL | Phase 4 (approved) | NR1I2 |
| AMLODIPINE | ChEMBL | Phase 4 (approved) | NR1I2 |
| AMSACRINE | ChEMBL | Phase 4 (approved) | NR1I2 |
| ATAZANAVIR | ChEMBL | Phase 4 (approved) | NR1I2 |
| BEDAQUILINE | ChEMBL | Phase 4 (approved) | NR1I2 |
| BENFLUOREX | ChEMBL | Phase 4 (approved) | NR1I2 |
| BENZBROMARONE | ChEMBL | Phase 4 (approved) | NR1I2 |
| BENZTHIAZIDE | ChEMBL | Phase 4 (approved) | NR1I2 |
| BEPRIDIL | ChEMBL | Phase 4 (approved) | NR1I2 |
| BETAMETHASONE DIPROPIONATE | ChEMBL | Phase 4 (approved) | NR1I2 |
| BIFONAZOLE | ChEMBL | Phase 4 (approved) | NR1I2 |
| BITHIONOL | ChEMBL | Phase 4 (approved) | NR1I2 |
| BRIMONIDINE | ChEMBL | Phase 4 (approved) | NR1I2 |
| BROMPERIDOL | ChEMBL | Phase 4 (approved) | NR1I2 |
| BUCLIZINE | ChEMBL | Phase 4 (approved) | NR1I2 |
| BUTENAFINE | ChEMBL | Phase 4 (approved) | NR1I2 |
| BUTOCONAZOLE | ChEMBL | Phase 4 (approved) | NR1I2 |
| CALCIPOTRIENE | ChEMBL | Phase 4 (approved) | NR1I2 |
| CALCITRIOL | ChEMBL | Phase 4 (approved) | NR1I2 |
| CANDESARTAN CILEXETIL | ChEMBL | Phase 4 (approved) | NR1I2 |
| CANNABIDIOL | ChEMBL | Phase 4 (approved) | NR1I2 |
| CAPSAICIN | ChEMBL | Phase 4 (approved) | NR1I2 |
| CARVEDILOL | ChEMBL | Phase 4 (approved) | NR1I2 |
| CEFACLOR | ChEMBL | Phase 4 (approved) | NR1I2 |
| CEFAMANDOLE | ChEMBL | Phase 4 (approved) | NR1I2 |
| CEFEPIME | ChEMBL | Phase 4 (approved) | NR1I2 |
| CEFMENOXIME | ChEMBL | Phase 4 (approved) | NR1I2 |
| CEFOTAXIME | ChEMBL | Phase 4 (approved) | NR1I2 |
| CEFOXITIN | ChEMBL | Phase 4 (approved) | NR1I2 |
| CEFPODOXIME | ChEMBL | Phase 4 (approved) | NR1I2 |
| CEFTAZIDIME | ChEMBL | Phase 4 (approved) | NR1I2 |
| CEFTIZOXIME | ChEMBL | Phase 4 (approved) | NR1I2 |
| CEFTRIAXONE | ChEMBL | Phase 4 (approved) | NR1I2 |
| CEFUROXIME | ChEMBL | Phase 4 (approved) | NR1I2 |
| CEPHALORIDINE | ChEMBL | Phase 4 (approved) | NR1I2 |
| CEPHALOTHIN | ChEMBL | Phase 4 (approved) | NR1I2 |
| CEPHAPIRIN | ChEMBL | Phase 4 (approved) | NR1I2 |
| CEPHRADINE | ChEMBL | Phase 4 (approved) | NR1I2 |
| CERIVASTATIN | ChEMBL | Phase 4 (approved) | HMGCR |
| CHLORHEXIDINE | ChEMBL | Phase 4 (approved) | NR1I2 |
| CHLOROXINE | ChEMBL | Phase 4 (approved) | NR1I2 |
| CHLORPROTHIXENE | ChEMBL | Phase 4 (approved) | NR1I2 |
| CICLESONIDE | ChEMBL | Phase 4 (approved) | NR1I2 |
| CICLOPIROX | ChEMBL | Phase 4 (approved) | NR1I2 |
| CISAPRIDE | ChEMBL | Phase 4 (approved) | HMGCR |
| CLEMASTINE | ChEMBL | Phase 4 (approved) | NR1I2 |
| CLOBETASOL PROPIONATE | ChEMBL | Phase 4 (approved) | NR1I2 |
| CLOPIDOGREL | ChEMBL | Phase 4 (approved) | NR1I2 |
| CLOTRIMAZOLE | ChEMBL | Phase 4 (approved) | NR1I2 |
| CYCLANDELATE | ChEMBL | Phase 4 (approved) | NR1I2 |
| DABIGATRAN ETEXILATE | ChEMBL | Phase 4 (approved) | NR1I2 |
| DABRAFENIB | ChEMBL | Phase 4 (approved) | NR1I2 |
| DACLATASVIR | ChEMBL | Phase 4 (approved) | NR1I2 |
| DANAZOL | ChEMBL | Phase 4 (approved) | NR1I2 |
| DAUNORUBICIN | ChEMBL | Phase 4 (approved) | NR1I2 |
| DEMECLOCYCLINE | ChEMBL | Phase 4 (approved) | NR1I2 |
| DESOGESTREL | ChEMBL | Phase 4 (approved) | NR1I2 |
| DESOXIMETASONE | ChEMBL | Phase 4 (approved) | NR1I2 |
| DIETHYLSTILBESTROL | ChEMBL | Phase 4 (approved) | NR1I2 |
| DIHYDROTACHYSTEROL | ChEMBL | Phase 4 (approved) | NR1I2 |
| DIMERCAPROL | ChEMBL | Phase 4 (approved) | NR1I2 |
| DINOPROSTONE | ChEMBL | Phase 4 (approved) | NR1I2 |
| DOMPERIDONE | ChEMBL | Phase 4 (approved) | NR1I2 |
| DRONABINOL | ChEMBL | Phase 4 (approved) | NR1I2 |
| DROXIDOPA | ChEMBL | Phase 4 (approved) | NR1I2 |
| EBASTINE | ChEMBL | Phase 4 (approved) | NR1I2 |
| ECONAZOLE | ChEMBL | Phase 4 (approved) | NR1I2 |
| EFAVIRENZ | ChEMBL | Phase 4 (approved) | NR1I2 |
| ENCORAFENIB | ChEMBL | Phase 4 (approved) | NR1I2 |
| ENZALUTAMIDE | ChEMBL | Phase 4 (approved) | NR1I2 |
| EPALRESTAT | ChEMBL | Phase 4 (approved) | NR1I2 |
| ETHINYL ESTRADIOL | ChEMBL | Phase 4 (approved) | NR1I2 |
| FEDRATINIB | ChEMBL | Phase 4 (approved) | NR1I2 |
| FELODIPINE | ChEMBL | Phase 4 (approved) | NR1I2 |
| FENTANYL | ChEMBL | Phase 4 (approved) | NR1I2 |
| FENTICONAZOLE | ChEMBL | Phase 4 (approved) | NR1I2 |
| FLUOROMETHOLONE | ChEMBL | Phase 4 (approved) | NR1I2 |
| FLUSPIRILENE | ChEMBL | Phase 4 (approved) | NR1I2 |
| FLUTICASONE PROPIONATE | ChEMBL | Phase 4 (approved) | NR1I2 |
| FLUTRIMAZOLE | ChEMBL | Phase 4 (approved) | NR1I2 |
Related Atlas pages
- Genes: NR1I2, HMGCR
- Indicated for: cardiovascular disorder, coronary artery disorder, atherosclerosis
- In clinical trials for: intermittent vascular claudication, myocardial ischemia, heart disorder, peripheral vascular disease, chronic obstructive pulmonary disease, HIV infectious disease, rheumatoid arthritis, melanoma, internal carotid artery stenosis, cerebral atherosclerosis, learning disability, breast neoplasm, ovarian cancer, arteriovenous malformations of the brain, Parkinson disease, cerebrotendinous xanthomatosis, fragile X syndrome, Rett syndrome, neurofibromatosis type 1, cerebrovascular disorder
- Drugs: Atorvastatin, Pitavastatin, Rosuvastatin, Simvastatin, Vorinostat, Bosentan, Crizotinib, Dacomitinib, Desoxycorticosterone Pivalate, Fulvestrant, Gefitinib, Pravastatin, Tadalafil, Abacavir, Acenocoumarol, Acetaminophen, Acitretin, Adapalene, Alectinib, Alpidem, Ambrisentan, Amlodipine, Amsacrine, Atazanavir, Bedaquiline, Benfluorex, Benzbromarone, Benzthiazide, Bepridil, Betamethasone Dipropionate, Bifonazole, Bithionol, Brimonidine, Bromperidol, Buclizine, Butenafine, Butoconazole, Calcipotriene, Calcitriol, Candesartan Cilexetil, Cannabidiol, Capsaicin, Carvedilol, Cefaclor, Cefamandole, Cefepime, Cefmenoxime, Cefotaxime, Cefoxitin, Cefpodoxime, Ceftazidime, Ceftizoxime, Ceftriaxone, Cefuroxime, Cephaloridine, Cephalothin, Cephapirin, Cephradine, Cerivastatin, Chlorhexidine, Chloroxine, Chlorprothixene, Ciclesonide, Ciclopirox, Cisapride, Clemastine, Clobetasol Propionate, Clopidogrel, Clotrimazole, Cyclandelate, Dabigatran Etexilate, Dabrafenib, Daclatasvir, Danazol, Daunorubicin, Demeclocycline, Desogestrel, Desoximetasone, Diethylstilbestrol, Dihydrotachysterol, Dimercaprol, Dinoprostone, Domperidone, Dronabinol, Droxidopa, Ebastine, Econazole, Efavirenz, Encorafenib, Enzalutamide, Epalrestat, Ethinyl Estradiol, Fedratinib, Felodipine, Fentanyl, Fenticonazole, Fluorometholone, Fluspirilene, Fluticasone Propionate, Flutrimazole