Ziconotide

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Also known as .omega.-conotoxin m viiaSNX-111Ziconotidaomega-Conotoxin

Summary

Ziconotide (CHEMBL4594214) is an approved protein (ATC N02BG08) targeting CACNA1A and CACNA1B; indicated across 2 conditions.

At a glance

  • Status: Approved (max clinical phase 4)
  • Modality: Protein
  • ATC class: N02BG08
  • Targets: 2 (CACNA1A, CACNA1B)
  • Indications: 2 conditions
  • Clinical trials: 10
  • Chemistry: 2639.2 Da · C102H172N36O32S7

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL4594214
NameZiconotide
TypeProtein
Max phase4
FDA approvedyes
PubChem CID16135415
ATCN02BG08
Molecular formulaC102H172N36O32S7
Molecular weight2639.2
InChIKeyBPKIMPVREBSLAJ-QTBYCLKRSA-N

SMILES: C[C@H]1C(=O)N[C@H](C(=O)N[C@H]2CSSC[C@H]3C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CSSC[C@@H](C(=O)N[C@@H](CSSC[C@@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)NCC(=O)N1)CCCCN)CCCCN)N)C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N3)CO)[C@@H](C)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC2=O)CO)CCCNC(=N)N)CC(C)C)CCSC)CC4=CC=C(C=C4)O)CC(=O)O)C(=O)N)CCCCN)CO)CCCNC(=N)N)CCCCN

IUPAC name: 2-[(1R,4S,7S,13S,16R,21R,24S,27S,30S,33S,36S,39S,42R,45S,48S,54S,60S,63R,68R,71S,77S)-63-amino-13,45,54,60-tetrakis(4-aminobutyl)-4,36-bis(3-carbamimidamidopropyl)-16-carbamoyl-71-[(1R)-1-hydroxyethyl]-7,39,77-tris(hydroxymethyl)-27-[(4-hydroxyphenyl)methyl]-48-methyl-33-(2-methylpropyl)-30-(2-methylsulfanylethyl)-2,5,8,11,14,23,26,29,32,35,38,41,44,47,50,53,56,59,62,69,72,75,78,85-tetracosaoxo-18,19,65,66,81,82-hexathia-3,6,9,12,15,22,25,28,31,34,37,40,43,46,49,52,55,58,61,70,73,76,79,84-tetracosazatricyclo[40.37.4.221,68]pentaoctacontan-24-yl]acetic acid

Also known as: .omega.-conotoxin m viia, SNX-111, Ziconotida, Ziconotide, omega-Conotoxin, ZICONOTIDE

Patent coverage: 545 distinct patent families (1,201 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 1,058 (88%) 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).

GeneTargetActionpAffinityCancer dependencyUniProt
CACNA1ACav2.1Antagonist6.30%O00555
CACNA1BCav2.2Antagonist10.3%Q00975

Broader ChEMBL bioactivity targets: 1 (assay-derived). Sample: Voltage-dependent N-type calcium channel subunit alpha-1B.

Bioactivity

ChEMBL activities: 2 potent at pChembl ≥ 5 of 2 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
CACNA1B6.3IC50500nMCHEMBL_ACT_1476708
CACNA1B6.22IC50600nMCHEMBL_ACT_1476707

Target pathways

Aggregated over 2 target gene(s): CACNA1A, CACNA1B.

Top Reactome pathways

6 total, by targets touching each:

PathwayTargetsGenes
Presynaptic depolarization and calcium channel opening2CACNA1A, CACNA1B
Transmission across Chemical Synapses2CACNA1A, CACNA1B
Neuronal System2CACNA1A, CACNA1B
Metabolism1CACNA1A
Integration of energy metabolism1CACNA1A
Regulation of insulin secretion1CACNA1A

Dominant GO biological processes

GO termTargets
chemical synaptic transmission2
modulation of chemical synaptic transmission2
calcium ion transmembrane transport2
calcium ion import across plasma membrane2
response to amyloid-beta2
monoatomic ion transport2
calcium ion transport2
monoatomic ion transmembrane transport2
transmembrane transport2
positive regulation of cytosolic calcium ion concentration1
cellular response to amyloid-beta1
positive regulation of calcium ion-dependent exocytosis of neurotransmitter1

Indications & clinical

Indications

2 indications (2 at ChEMBL trial phase 4).

The 2 indication records carry no mapped disease name (EFO/MeSH-only); none shown.

Clinical trials

Total trials: 10.

Phase distribution

PhaseTrials
Not specified4
PHASE43
PHASE22
PHASE31

Top trials by phase / activity

NCTPhaseStatusTitle
NCT01373983PHASE4COMPLETEDIntrathecal Bolus Doses of Ziconotide
NCT01992562PHASE4WITHDRAWNSingle Shot Intrathecal Ziconotide for Painful Neuropathy or Myelopathy
NCT03321955PHASE4COMPLETEDZiconotide as First-Line IDT
NCT00076544PHASE3COMPLETEDZiconotide Effectiveness and Safety Trial in Patients With Chronic Severe Pain
NCT00002160PHASE2COMPLETEDA Multicenter Phase II/III, Placebo-Controlled Study of SNX-111 Administered Intrathecally to Cancer and AIDS Patients With Chronic Pain
NCT00996983PHASE2UNKNOWNSafety and Activity Study of Intrathecally Administered Ziconotide for Neuropathic Pain in Patients With Cancer
NCT04321408Not specifiedRECRUITINGOP2C : Prialt® Observatory in Clinical Practice
NCT06541184Not specifiedRECRUITINGZiconotide for Non-cancer Pain by Intrathecal Administration
NCT07499882Not specifiedNOT_YET_RECRUITINGIntrathecal Ziconotide in Chemotherapy Induced Peripheral Neuropathy
NCT01888120Not specifiedCOMPLETEDPatient Registry of Intrathecal Ziconotide Management(PRIZM)

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No PharmGKB pharmacogenomic data curated for this drug.

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.

25 molecules share ≥1 primary target. Top 25 by shared-target count:

MoleculeSourceStatusShared targets
NifedipineChEMBL + PubChemPhase 4 (approved)CACNA1A, CACNA1B
NIMODIPINEChEMBL + PubChemPhase 4 (approved)CACNA1A, CACNA1B
TACRINEChEMBLPhase 4 (approved)CACNA1A, CACNA1B
AMITRIPTYLINEChEMBL + PubChemPhase 4 (approved)CACNA1B
AMOXAPINEChEMBL + PubChemPhase 4 (approved)CACNA1B
CLOMIPRAMINEChEMBL + PubChemPhase 4 (approved)CACNA1B
CYCLOBENZAPRINEChEMBL + PubChemPhase 4 (approved)CACNA1B
DESIPRAMINEChEMBL + PubChemPhase 4 (approved)CACNA1B
IMIPRAMINEChEMBL + PubChemPhase 4 (approved)CACNA1B
MAPROTILINEChEMBLPhase 4 (approved)CACNA1B
MIBEFRADILChEMBLPhase 4 (approved)CACNA1B
NORTRIPTYLINEChEMBLPhase 4 (approved)CACNA1B
PROMETHAZINEChEMBLPhase 4 (approved)CACNA1B
PROTRIPTYLINEChEMBLPhase 4 (approved)CACNA1B
TRIMIPRAMINEChEMBLPhase 4 (approved)CACNA1B
CILNIDIPINEChEMBLPhase 3CACNA1B
HESPERIDINChEMBLPhase 3CACNA1B
OPIPRAMOLChEMBLPhase 3CACNA1B
FLUNARIZINEChEMBLPhase 2CACNA1B
LOMERIZINEChEMBLPhase 2CACNA1B
SELICICLIBChEMBLPhase 2CACNA1B
Z160ChEMBLPhase 2CACNA1B
ClotrimazolePubChemApprovedCACNA1B
EconazolePubChemApprovedCACNA1B
MiconazolePubChemApprovedCACNA1B