Paricalcitol
drugOn this page
Also known as COMPOUND 49510COMPOUND-49510ZemplarSID144206540
Summary
Paricalcitol (CHEMBL1200622) is an approved small-molecule antiparathyroid drug (ATC H05BX02) targeting VDR; indicated across 21 conditions including chronic kidney disease and secondary hyperparathyroidism.
At a glance
- Status: Approved (max clinical phase 4)
- Modality: Small molecule
- ATC class: H05BX02
- Targets: 1 (VDR)
- Indications: 21 conditions
- Clinical trials: 88
- Chemistry: 416.6 Da · C27H44O3
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL1200622 |
| Name | Paricalcitol |
| Type | Small molecule |
| Max phase | 4 |
| FDA approved | yes |
| PubChem CID | 5281104 |
| ChEBI | CHEBI:7931 |
| ATC | H05BX02 |
| Molecular formula | C27H44O3 |
| Molecular weight | 416.6 |
| InChIKey | BPKAHTKRCLCHEA-UBFJEZKGSA-N |
SMILES: C[C@H](/C=C/[C@H](C)C(C)(C)O)[C@H]1CC[C@@H]\2[C@@]1(CCC/C2=C\C=C3C[C@H](C[C@@H](C3)O)O)C
IUPAC name: trans-(1R,3R)-5-[(2E)-2-[(1R,3aS,7aR)-1-[(E,2R,5S)-6-hydroxy-5,6-dimethylhept-3-en-2-yl]-7a-methyl-2,3,3a,5,6,7-hexahydro-1H-inden-4-ylidene]ethylidene]cyclohexane-1,3-diol
Pharmacological roles (ChEBI): antiparathyroid drug.
Also known as: COMPOUND 49510, COMPOUND-49510, Paricalcitol, Zemplar, PARICALCITOL, paricalcitol, SID144206540
Patent coverage: 1,133 distinct patent families (4,394 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 |
|---|---|---|---|---|---|
| VDR | Vitamin D receptor | Agonist | 0.2% | P11473 |
Bioactivity
No ChEMBL bioactivity rows at pChembl ≥ 5 (expected for biologics / antibodies).
Target pathways
Aggregated over 1 target gene(s): VDR.
Top Reactome pathways
3 total, by targets touching each:
| Pathway | Targets | Genes |
|---|---|---|
| Vitamin D (calciferol) metabolism | 1 | VDR |
| Nuclear Receptor transcription pathway | 1 | VDR |
| SUMOylation of intracellular receptors | 1 | VDR |
Dominant GO biological processes
| GO term | Targets |
|---|---|
| negative regulation of transcription by RNA polymerase II | 1 |
| cell morphogenesis | 1 |
| skeletal system development | 1 |
| calcium ion transport | 1 |
| intracellular calcium ion homeostasis | 1 |
| lactation | 1 |
| negative regulation of cell population proliferation | 1 |
| positive regulation of gene expression | 1 |
| negative regulation of keratinocyte proliferation | 1 |
| cell differentiation | 1 |
| positive regulation of bone mineralization | 1 |
| intracellular receptor signaling pathway | 1 |
| phosphate ion transmembrane transport | 1 |
| nuclear receptor-mediated bile acid signaling pathway | 1 |
| mRNA transcription by RNA polymerase II | 1 |
Indications & clinical
Indications
21 indications (3 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).
| Indication | Trial phase | MONDO | EFO |
|---|---|---|---|
| chronic kidney disease | 4 | MONDO:0005300 | EFO:0003884 |
| secondary hyperparathyroidism | 4 | MONDO:0006964 | EFO:1001173 |
| parathyroid gland disorder | 4 | MONDO:0001223 | EFO:0005754 |
| IgA glomerulonephritis | 3 | MONDO:0005342 | EFO:0004194 |
| proteinuria | 3 | MONDO:0003634 | HP:0000093 |
| kidney disorder | 3 | MONDO:0005240 | EFO:0003086 |
| hyperparathyroidism | 3 | MONDO:0001741 | EFO:0008506 |
| exocrine pancreatic carcinoma | 2 | MONDO:0005192 | EFO:0002618 |
| diabetic kidney disease | 2 | MONDO:0005016 | EFO:0000401 |
| type 2 diabetes mellitus | 2 | MONDO:0005148 | MONDO:0005148 |
| malignant pancreatic neoplasm | 2 | MONDO:0009831 | EFO:1000359 |
| pancreatic ductal adenocarcinoma | 2 | MONDO:0005184 | MONDO:0005184 |
| neoplasm | 1 | MONDO:0005070 | EFO:0000616 |
| plasma cell myeloma | 1 | MONDO:0009693 | EFO:0001378 |
| breast neoplasm | 1 | MONDO:0021100 | MONDO:0007254 |
| plasma cell neoplasm | 1 | MONDO:0004959 | EFO:0000200 |
| chronic pancreatitis | 0 | MONDO:0005003 | EFO:0000342 |
4 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.
Clinical trials
Total trials: 88.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE4 | 23 |
| PHASE3 | 20 |
| PHASE2 | 20 |
| Not specified | 11 |
| PHASE1 | 10 |
| EARLY_PHASE1 | 3 |
| PHASE2/PHASE3 | 1 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT00053547 | PHASE4 | COMPLETED | Safety and Effectiveness of Zemplar Injection in Decreasing iPTH Levels in Pediatric ESRD Subjects on Hemodialysis |
| NCT00073710 | PHASE4 | COMPLETED | Study to Evaluate the Effects of Zemplar Injection and Calcijex on Intestinal Absorption of Calcium |
| NCT00091481 | PHASE4 | COMPLETED | Study to Compare Initial Dosing Parameters of Zemplar in Stage V Chronic Kidney Disease Subjects on Hemodialysis |
| NCT00294866 | PHASE4 | COMPLETED | Effect of Paricalcitol on Markers of Inflammation in Hemodialysis Patients |
| NCT00307840 | PHASE4 | COMPLETED | Initial Dosing of Paricalcitol in Secondary Hyperparathyroidism |
| NCT00537979 | PHASE4 | COMPLETED | Efficacy and Safety of 6 Months Treatment With Paricalcitol Injection or Oral in Patients With Secondary Hyperparathyroidism on Dialysis |
| NCT00664430 | PHASE4 | TERMINATED | Efficacy and Safety of Paricalcitol on the Treatment of Secondary Hyperparathyroidism in Calcitriol Resistant Dialysis Subjects |
| NCT00752102 | PHASE4 | COMPLETED | Vitamin D and Coronary Calcification Study |
| NCT00823303 | PHASE4 | COMPLETED | Paricalcitol Versus Calcitriol for Efficacy and Safety in Stage 3/4 Chronic Kidney Disease (CKD) With Secondary Hyperparathyroidism (SHPT) |
| NCT00891813 | PHASE4 | COMPLETED | Effectiveness and Safety of IV Zemplar in Patients on Hemodialysis and With Secondary Hyperparathyroidism Using iPTH/100 as Initial Dose |
| NCT00958451 | PHASE4 | COMPLETED | Vitamin D Deficiency in Chronic Kidney Disease (CKD) Patients |
| NCT00977080 | PHASE4 | COMPLETED | Evaluation of the Effectiveness of Paricalcitol Versus Cinacalcet With Low-Dose Vitamin D |
| NCT01163162 | PHASE4 | COMPLETED | The Effect of Paricalcitol on Creatinine Filtration, Secretion and Glomerular Filtration Rate |
| NCT01265615 | PHASE4 | COMPLETED | Paricalcitol Versus Calcitriol for the Management of Renocardiac Syndrome in Renal Transplant Patients |
| NCT01331317 | PHASE4 | COMPLETED | Effect of a Vitamin D Analogue vs Placebo on p-NT-proBNP in Patients With Type 1 DM and Diabetic Nephropathy |
| NCT01506947 | PHASE4 | COMPLETED | A Pilot Clinical Study Evaluating the Effect of Parathyroid Hormone (PTH) Lowering On Erythropoietin Consumption in Calcitriol-Resistant Patients |
| NCT01725113 | PHASE4 | TERMINATED | Management of Mineral and Bone Disease in Hemodialysis-Calcitriol vs. Paricalcitol |
| NCT01768351 | PHASE4 | COMPLETED | Paricalcitol Effect on Anemia in CKD |
| NCT01939977 | PHASE4 | COMPLETED | Efficacy and Safety of Paricalcitol in the Reduction of Secondary Hyperparathyroidism After Kidney Transplantation. |
| NCT02372695 | PHASE4 | TERMINATED | Effect of Paricalcitol Over Vessel Wall |
| NCT02876211 | PHASE4 | TERMINATED | Paricalcitol Improves Anemia of Inflammation |
| NCT03023748 | PHASE4 | UNKNOWN | Intravenous Paricalcitol in Chronic Hemodialysis Patients |
| NCT03588884 | PHASE4 | COMPLETED | Repeated-dose Safety, Efficacy, Pharmacokinetic and Pharmacodynamic of CTAP101, Immediate-release Calcifediol, High-dose Cholecalciferol, and Paricalcitol Plus Low-dose Cholecalciferol in Patients With Secondary Hyperparathyroidism, Chronic Kidney Disease 3-4 and Vitamin D Insufficiency |
| NCT00048438 | PHASE3 | COMPLETED | Safety and Efficacy of Zemplar Capsule in Reducing Serum IPTH Levels in Chronic Kidney Disease Subjects (Three Times Weekly) |
| NCT00048451 | PHASE3 | COMPLETED | Safety and Efficacy of Zemplar Capsule in Reducing Serum iPTH Levels in Chronic Kidney Disease Subjects (Three Times Weekly) |
| NCT00048516 | PHASE3 | COMPLETED | Safety and Efficacy of Zemplar Capsule in Reducing Serum iPTH Levels in Chronic Kidney Disease Subjects (Daily Dosing) |
| NCT00091975 | PHASE3 | COMPLETED | Zemplar® Capsule in Reducing Serum Intact Parathyroid Hormone Levels in Chronic Kidney Disease Stage 5 Subjects on Hemodialysis or Peritoneal Dialysis |
| NCT00417612 | PHASE3 | COMPLETED | Effectiveness of Paricalcitol in Reducing Parathyroid Hormone (PTH) Levels in X-linked Hypophosphatemic Rickets |
| NCT00497146 | PHASE3 | COMPLETED | The PRIMO Study: Paricalcitol Capsules Benefits Renal Failure Induced Cardiac Morbidity in Subjects With Chronic Kidney Disease Stage 3/4 |
| NCT00599963 | PHASE3 | WITHDRAWN | Paricalcitol for the Treatment of Immunoglobulin A Nephropathy |
| NCT00646035 | PHASE3 | COMPLETED | A Study to Evaluate the Safety and Efficacy of Paricalcitol Capsules in Reducing Serum Intact Parathyroid Hormone Levels in End Stage Renal Disease Subjects on Peritoneal Dialysis |
| NCT01012414 | PHASE3 | TERMINATED | Effect of Vitamin D Supplement on Inflammation Markers in High-Risk Cardiovascular Patients With Chronic Kidney Disease |
| NCT01020487 | PHASE3 | COMPLETED | Safety and Efficacy of Paricalcitol Capsules in Decreasing Serum Parathyroid Hormone Levels in Children Aged 10-16 With Chronic Kidney Disease (CKD) |
| NCT01071070 | PHASE3 | COMPLETED | Evaluate Safety and Efficacy of Paricalcitol in Reducing Serum Intact Parathyroid Hormone in Chronic Kidney Disease |
| NCT01138475 | PHASE3 | COMPLETED | Trial Of Paricalcitol and Cholecalciferol(Vitamin D3) in the Treatment Of Secondary Hyperparathyroidism in Patients After ROUX-EN-Y Gastric Bypass Surgery |
| NCT01204528 | PHASE2/PHASE3 | COMPLETED | Vitamin-D Receptor Activation (VDRA) in Chronic Kidney Disease |
| NCT01341782 | PHASE3 | COMPLETED | Comparison of Efficacy and Safety of Paricalcitol Injection With Maxacalcitol Injection in Adult Japanese Chronic Kidney Disease Subjects Receiving Hemodialysis With Secondary Hyperparathyroidism |
| NCT01382212 | PHASE3 | COMPLETED | A Study to Evaluate the Safety of Paricalcitol Capsules in Pediatric Subjects Ages 10 to 16 With Stage 5 Chronic Kidney Disease Receiving Peritoneal Dialysis or Hemodialysis |
| NCT01436747 | PHASE3 | COMPLETED | Efficacy and Safety of Paricalcitol for Reduction of Proteinuria in Kidney Transplant Recipients |
| NCT01694160 | PHASE3 | COMPLETED | Oral Paricalcitol in Renal Transplant Recipients for Reducing Albuminuria |
Clinical evidence (CIViC)
No CIViC predictive evidence (expected for non-precision-medicine drugs).
Pharmacology
Pharmacogenomics
No CPIC/DPWG dosing guideline or drug-level clinical/variant annotations in PharmGKB for this molecule.
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.
10 molecules share ≥1 primary target. Top 10 by shared-target count:
| Molecule | Source | Status | Shared targets |
|---|---|---|---|
| CALCIPOTRIENE | ChEMBL | Phase 4 (approved) | VDR |
| CALCITRIOL | ChEMBL | Phase 4 (approved) | VDR |
| CHOLECALCIFEROL | ChEMBL | Phase 4 (approved) | VDR |
| DOXERCALCIFEROL | ChEMBL | Phase 4 (approved) | VDR |
| TACALCITOL | ChEMBL | Phase 4 (approved) | VDR |
| CURCUMIN | ChEMBL | Phase 3 | VDR |
| MAXACALCITOL | ChEMBL | Phase 3 | VDR |
| SEOCALCITOL | ChEMBL | Phase 3 | VDR |
| TAUROLITHOCHOLIC ACID | ChEMBL | Phase 3 | VDR |
| chenodiol | PubChem | Approved | VDR |
Related Atlas pages
- Genes: VDR
- Diseases: chronic kidney disease, secondary hyperparathyroidism, parathyroid gland disorder, IgA glomerulonephritis, proteinuria, kidney disorder, hyperparathyroidism
- Drugs: Calcipotriene, Calcitriol, Cholecalciferol, Doxercalciferol, Tacalcitol, Curcumin, Maxacalcitol, Seocalcitol, Taurolithocholic Acid, chenodiol