Ziconotide (PRIALT; SNX-111) is a neuroactive peptide, which was approved by FDA in 2004 for the management of severe chronic pain in adult patients for whom intrathecal therapy is warranted, and who are intolerant of or refractory to other treatment, such as systemic analgesics, adjunctive therapies, or intrathecal morphine. Ziconotide acts as a selective N-type voltage-gated calcium channel blocker, which leads to a blockade of excitatory neurotransmitter release from the primary afferent nerve terminals.
CNS Activity
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: Voltage-dependent N-type calcium channels |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Primary | PRIALT Approved UsePRIALT (ziconotide) solution, intrathecal infusion is an N-type calcium channel antagonist indicated for the management of severe chronic pain in patients for whom intrathecal therapy is warranted, and who are intolerant of or refractory to other treatment, such as systemic analgesics, adjunctive therapies, or intrathecal morphine. Launch Date2004 |
PubMed
| Title | Date | PubMed |
|---|---|---|
| Pharmacological Inhibition of Voltage-gated Ca(2+) Channels for Chronic Pain Relief. | 2013-12 |
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| Mechanisms of conotoxin inhibition of N-type (Ca(v)2.2) calcium channels. | 2013-07 |
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| Pharmacological characterization of recombinant N-type calcium channel (Cav2.2) mediated calcium mobilization using FLIPR. | 2006-09-14 |
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| Ziconotide: neuronal calcium channel blocker for treating severe chronic pain. | 2004-12 |
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| Identification and characterization of novel human Ca(v)2.2 (alpha 1B) calcium channel variants lacking the synaptic protein interaction site. | 2002-01-01 |
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| Novel omega-conotoxins from Conus catus discriminate among neuronal calcium channel subtypes. | 2000-11-10 |
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| Pharmacotherapeutic potential of omega-conotoxin MVIIA (SNX-111), an N-type neuronal calcium channel blocker found in the venom of Conus magus. | 1998-11 |
|
| Neuronal calcium channel antagonists. Discrimination between calcium channel subtypes using omega-conotoxin from Conus magus venom. | 1987-04-21 |
Sample Use Guides
PRIALT (ziconotide) solution is intended for administration by or under the direction of a physician experienced in the technique of intrathecal administration and who is familiar with the drug and device labeling. PRIALT may be used for therapy undiluted (25 mcg/mL in 20 mL vial) or diluted (100 mcg/mL in 1 or 5 mL vials). The 100 mcg/mL formulation may be administered undiluted once an appropriate dose has been established.
Route of Administration:
Other
| Substance Class |
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EMA ASSESSMENT REPORTS |
PRIALT (AUTHORIZED: INJECTIONS, SPINAL)
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ACTIVE MOIETY |
Structural Modifications
| Modification Type | Location Site | Location Type | Residue Modified | Extent | Fragment Name | Fragment Approval |
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| MOIETY | Acetic acid | Q40Q9N063P | ||||
| AMINO ACID SUBSTITUION | [1_25] | CYSTEINAMIDE | 055X467671 |
| Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
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| Molecular Formula | CHEMICAL |
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| MOL_WEIGHT:SEQUENCE(CALCULATED) | CHEMICAL |
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