Etelcalcetide
drugOn this page
Also known as EtelcalcetidaKAI-4169ONO-5163TelcalcetideVelcalcetide
Summary
Etelcalcetide (CHEMBL3545184) is an approved protein (ATC H05BX04) targeting CASR; indicated across 3 conditions including secondary hyperparathyroidism and parathyroid gland disorder.
At a glance
- Status: Approved (max clinical phase 4)
- Modality: Protein
- ATC class: H05BX04
- Targets: 1 (CASR)
- Indications: 3 conditions
- Clinical trials: 18
- Chemistry: 1048.3 Da · C38H73N21O10S2
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL3545184 |
| Name | Etelcalcetide |
| Type | Protein |
| Max phase | 4 |
| FDA approved | yes |
| PubChem CID | 71511839 |
| ATC | H05BX04 |
| Molecular formula | C38H73N21O10S2 |
| Molecular weight | 1048.3 |
| InChIKey | ANIAZGVDEUQPRI-ZJQCGQFWSA-N |
SMILES: C[C@H](C(=O)N[C@H](CCCN=C(N)N)C(=O)N)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@@H](C)NC(=O)[C@@H](CSSC[C@@H](C(=O)O)N)NC(=O)C
IUPAC name: (2R)-3-[[(2S)-2-acetamido-3-[[(2R)-1-[[(2R)-1-[[(2R)-1-[[(2R)-1-[[(2R)-1-[[(2R)-1-amino-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-oxopropyl]disulfanyl]-2-aminopropanoic acid
Also known as: Etelcalcetida, Etelcalcetide, KAI-4169, ONO-5163, Telcalcetide, Velcalcetide, ETELCALCETIDE
Parent form; salt/anhydrous children: CHEMBL3545183
Patent coverage: 265 distinct patent families (575 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 469 (82%) of the total. 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 |
|---|---|---|---|---|---|
| CASR | CaS receptor | Positive | 4.6 | 0.1% | P41180 |
Bioactivity
No ChEMBL bioactivity rows at pChembl ≥ 5 (expected for biologics / antibodies).
Target pathways
Aggregated over 1 target gene(s): CASR.
Top Reactome pathways
7 total, by targets touching each:
| Pathway | Targets | Genes |
|---|---|---|
| Signal Transduction | 1 | CASR |
| Signaling by GPCR | 1 | CASR |
| GPCR downstream signalling | 1 | CASR |
| G alpha (q) signalling events | 1 | CASR |
| G alpha (i) signalling events | 1 | CASR |
| Class C/3 (Metabotropic glutamate/pheromone receptors) | 1 | CASR |
| GPCR ligand binding | 1 | CASR |
Dominant GO biological processes
| GO term | Targets |
|---|---|
| ossification | 1 |
| response to ischemia | 1 |
| detection of calcium ion | 1 |
| intracellular calcium ion homeostasis | 1 |
| G protein-coupled receptor signaling pathway | 1 |
| adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway | 1 |
| phospholipase C-activating G protein-coupled receptor signaling pathway | 1 |
| JNK cascade | 1 |
| chemosensory behavior | 1 |
| positive regulation of cell population proliferation | 1 |
| anatomical structure morphogenesis | 1 |
| positive regulation of gene expression | 1 |
| positive regulation of insulin secretion | 1 |
| bile acid secretion | 1 |
| cellular response to hepatocyte growth factor stimulus | 1 |
Indications & clinical
Indications
3 indications (2 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 |
|---|---|---|---|
| secondary hyperparathyroidism | 4 | MONDO:0006964 | EFO:1001173 |
| parathyroid gland disorder | 4 | MONDO:0001223 | EFO:0005754 |
| chronic kidney disease | 1 | MONDO:0005300 | EFO:0003884 |
Clinical trials
Total trials: 18.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE3 | 9 |
| PHASE2 | 5 |
| PHASE1 | 4 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT03633708 | PHASE3 | RECRUITING | A Trial of Etelcalcetide in Pediatric Participants With Secondary Hyperparathyroidism and Chronic Kidney Disease on Hemodialysis |
| NCT03969329 | PHASE3 | RECRUITING | A Phase 3 Study of Etelcalcetide in Children With Secondary Hyperparathyroidism Receiving Hemodialysis |
| NCT01785849 | PHASE3 | COMPLETED | Efficacy and Safety of Etelcalcetide (AMG 416) in the Treatment of Secondary Hyperparathyroidism (SHPT) in Patients With Chronic Kidney Disease on Hemodialysis |
| NCT01785875 | PHASE3 | COMPLETED | Extension Study of Etelcalcetide in the Treatment of Secondary Hyperparathyroidism (SHPT) in Patients With Chronic Kidney Disease (CKD) on Hemodialysis |
| NCT01788046 | PHASE3 | COMPLETED | Efficacy and Safety of Etelcalcetide (AMG 416) in the Treatment of Secondary Hyperparathyroidism (SHPT) in Patients With Chronic Kidney Disease (CKD) on Hemodialysis |
| NCT01896232 | PHASE3 | COMPLETED | Head-to-Head Study of Etelcalcetide (AMG 416) and Cinacalcet |
| NCT01932970 | PHASE3 | COMPLETED | Study to Assess the Impact on Calcium Levels When Hemodialysis Patients With Secondary Hyperparathyroidism (SHPT) Switch From Cinacalcet to Etelcalcetide |
| NCT02102204 | PHASE3 | COMPLETED | Extension Study of Etelcalcetide for Treatment of Secondary Hyperparathyroidism in Patients With Chronic Kidney Disease on Hemodialysis |
| NCT03299244 | PHASE3 | COMPLETED | Head-to-Head Study of Etelcalcetide and Cinacalcet in Asian Hemodialysis Patients With Secondary Hyperparathyroidism (SHPT) |
| NCT01254565 | PHASE2 | COMPLETED | Safety, Tolerability and Efficacy of Etelcalcetide in Hemodialysis Patients With Secondary Hyperparathyroidism |
| NCT01414114 | PHASE2 | COMPLETED | Etelcalcetide to Treat Secondary Hyperparathyroidism in Hemodialysis Patients With Chronic Kidney Disease-Mineral and Bone Disorder |
| NCT01576146 | PHASE2 | TERMINATED | Open-label Study to Assess the Long-term Safety and Efficacy of Etelcalcetide (Also Known as AMG 416 or KAI-4169) in Patients With Secondary Hyperparathyroidism |
| NCT03795558 | PHASE2 | COMPLETED | A Study to Investigate the Influence of PTH-lowering by Etelcalcetide (Parsabiv®) on the Calcification Propensity of Serum in Dialysis Patients |
| NCT03960437 | PHASE2 | COMPLETED | The Effect of Etelcalcetide on CKD-MBD |
| NCT01134549 | PHASE1 | COMPLETED | Safety, Tolerability and Pharmacokinetics of Etelcalcetide in Healthy Male Volunteers |
| NCT01134562 | PHASE1 | COMPLETED | Safety, Tolerability and Pharmacokinetics of Etelcalcetide in Hemodialysis Patients With Secondary Hyperparathyroidism |
| NCT02833857 | PHASE1 | COMPLETED | A Single-dose Study in Paediatric Patients Aged 2 to Less Than 18 Years With Secondary Hyperparathyroidism (sHPT) Receiving Haemodialysis |
| NCT03283098 | PHASE1 | COMPLETED | A Phase 1 Study to Evaluate PK, Safety and Tolerability of AMG 416 |
Clinical evidence (CIViC)
No CIViC predictive evidence (expected for non-precision-medicine drugs).
Pharmacology
Pharmacogenomics
No PharmGKB pharmacogenomic data curated for this drug.
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.
8 molecules share ≥1 primary target. Top 8 by shared-target count:
| Molecule | Source | Status | Shared targets |
|---|---|---|---|
| CINACALCET | ChEMBL + PubChem | Phase 4 (approved) | CASR |
| ENCALERET | ChEMBL | Phase 3 | CASR |
| EVOCALCET | ChEMBL | Phase 3 | CASR |
| FENDILINE | ChEMBL | Phase 2 | CASR |
| RONACALERET | ChEMBL | Phase 2 | CASR |
| SB-423562 | ChEMBL | Phase 2 | CASR |
| TECALCET | ChEMBL | Phase 2 | CASR |
| tryptophan | PubChem | Approved | CASR |
Related Atlas pages
- Genes: CASR
- Diseases: secondary hyperparathyroidism, parathyroid gland disorder
- Drugs: Cinacalcet, Encaleret, Evocalcet, tryptophan