Na+ channels (Sodium Channels) are proteins, which initiate the action potentials in neurons and other excitable cells. Na+ channel blockers impair the conduction of sodium ions through sodium channels. Some of the sodium channel blockers act by blocking sodium channels by binding to and occluding the extracellular pore opening of the channel, where as some drugs block sodium channels from the intracellular side of the channel. Intracellular blocking of the sodium channels is done by local anaesthetics, class I antiarrhytmatic agents, and anticonvulsants. Na+ channel antagonists are used as anaesthetics in both pre- and post-operative conditions, they are also used for supraventricular tachycardia, ventricular tachycardia, in prevention of ventricular fibrillation as antiarrythmatic agents, and in epileptic patients as anticonvulsants. Sanofi, AstraZeneca, Gilead Sciences, AbbiVie, Heron Therapeutics are some of the major players in the Na+ channel antagonist market.
Key Market Developments:
- In Dec 2020, Supermas received patent protection for Topiramate ER in the USA, Mexico, Australia, Japan, Canada, and Europe.
- In Dec 2020, Supermas entered into a collaboration agreement with Stendhal Mexico for commercialization of Oxcarbazeoine ER outside of the USA.
- In Mar 2023, Lee’s Pharmaceuticals registered Lidocaine transdermal for anaesthesia in children in China.
- In Aug 2022, Scilex Holding received a Fast Track designation for back pain in elderly and adults in the USA.
Approved Drug Molecules and Brand Names for Na+ channel Antagonists:
- Chirocaine (Levobupivacaine)
- Exparel (Bupivacaine liposome injectable suspension)
- Topiramate
- Lignocaine
- Lacosamide
- Ranolazine ER
- Phenytoin
- Zonisamide
- Aptiom (Eslicarbazepine)
- Flecainide
- Lidocaine 5%
- Emla-Cream
- Multaq (Dronedarone)
- Mexiletine
- Brinavess (Vernakalant)
- Zynrelef (Bupivacaine/Meloxicam ER)
- Pliaglis (Lidocaine and Tetracaine topical cream 7%)
- Xcopri (Cenobamate)
- Deudextromethorphan Quinidine ultra-low dose (AVP-786)
- ZTlido (Lidocaine patch 1.8%)
- Posimir (Bupivacaine CR)
- Fortacin (Lidocaine/Prilocaine spray)
- Alenura (Lidocaine/Heparin)
- Topiramate XR
- Quinidine sulfate
- Penles Tape (Lidocaine)
- Lidocaine Epinephrine transdermal
Drugs under the Pipeline for Na+ channel Antagonists:
- AZD1305
- Eleclazine (GS-6615)
- Omzya (Tolperisone immediate release)
- LiRIS (Lidocaine)
- Urolieve (Lidocaine Alkalized Intravesicular)
- BI 1265162
- Etoreat (Etodolac/Lidocaine patch)
- Celivarone (SSR149744C)
- Ropivacaine Liposomal sustained release (HR18034)
- Bupivacaine buccal (Oracain)
- Bupivacaine dextrose
- Flecainide inhalation (InRhythm)
- Ropivacaine extended-release oily solution (PRF-110)
- Topiramate XR
- Lidbree (Lidocaine topical gel)
- P-321
- Ropivacaine Liposomal (TLC590)
- ASN008
- Eladur (Bupivacaine)
- Ztlido 5.4% (Lidocaine topical patch 5.4%)
- Budiodarone (ATI-2042)
- Bupivacaine Microsphere (ND-340)
- Lidocaine gel (CNTX-2022)
- AZD3161
- AZD7009
- Versatis LE (Lidocaine/Diclofenac Epolamine FDC patch)
- Bupivacaine implant (ATX-101)
- Bupivacaine Pamoate microparticle suspension (HYR-PB21)
- Bupivacaine topical spray (GTX-101)
- Lamotrigine/Sertraline (LAMSER)
- Lidocaine (ARC-2022)
- Lidocaine bioadhesive gel, 10% (COL-1077)
- Lidocaine sustained release (ST-01)
- Lidocaine topical spray 5% solution (APC101)
- Neosaxitoxin (NeoSTX)
- Ranolazine/Dronedarone
- Ropivacaine depot (F-93)
Clinical Activity and Developments of Na+ channel Antagonists:
Currently, there are 65 drug products in Na+ channel antagonists, including 27 approved ones, and more than 30 drug molecules in clinical trials.
- In Mar 2023, UCB completed the phase-III VALUE trial for Lacosamide in generalized seizures in the USA, Australia, Brazil, South Korea, Israel, Russia, Turkey, Taiwan, Japan, Mexico, Bulgaria, Belgium, China, Czech Republic, France, Germany, Hungary, and others.
- In Mar 2022, Neurana Pharmaceuticals completed the phase-III RESUME-1 trial for back pain in the USA for Tolperisone.
|
Molecule Name |
Number of Studies |
|
AZD1305 |
13 |
|
Eleclazine (GS-6615) |
10 |
|
Omzya (Tolperisone immediate release) |
9 |
|
LiRIS (Lidocaine) |
6 |
|
Urolieve (Lidocaine Alkalized Intravesicular) |
6 |
|
BI 1265162 |
5 |
|
Etoreat (Etodolac/Lidocaine patch) |
|
|
Celivarone (SSR149744C) |
5 |
|
Ropivacaine Liposomal sustained release (HR18034) |
5 |
|
Bupivacaine buccal (Oracain) |
5 |
|
Bupivacaine dextrose |
4 |
|
Flecainide inhalation (InRhythm) |
4 |
|
Ropivacaine extended-release oily solution (PRF-110) |
4 |
|
Topiramate XR |
4 |
|
Lidbree (Lidocaine topical gel) |
3 |
|
P-321 |
3 |
|
Ropivacaine Liposomal (TLC590) |
3 |
|
ASN008 |
2 |
|
Eladur (Bupivacaine) |
2 |
|
Ztlido 5.4% (Lidocaine topical patch 5.4%) |
2 |
|
Budiodarone (ATI-2042) |
2 |
|
Bupivacaine microsphere (ND-340) |
2 |
|
Lidocaine gel (CNTX-2022) |
2 |
|
AZD3161 |
1 |
|
AZD7009 |
1 |
|
Versatis LE (Lidocaine/Diclofenac Epolamine FDC patch) |
1 |
|
Bupivacaine implant (ATX-101) |
1 |
|
Bupivacaine pamoate microparticle suspension (HYR-PB21) |
1 |
|
Bupivacaine topical spray (GTX-101) |
1 |
|
Lamotrigine/Sertraline (LAMSER) |
1 |
|
Lidocaine (ARC-2022) |
1 |
|
Lidocaine bioadhesive gel, 10% (COL-1077) |
1 |
|
Lidocaine sustained release (ST-01) |
1 |
|
Lidocaine topical spray 5% solution (APC101) |
1 |
|
Neosaxitoxin (NeoSTX) |
1 |
|
Ranolazine/Dronedarone |
1 |
|
Ropivacaine depot (F-93) |
1 |
Target Indication Analysis of Na+ channel Antagonists
Na+ channel blockers such as Levobupivacaine and Mepivacaine are used for anesthesia, postoperative pain. Topiramte is indicated in epilepsy, Lennox-Gastaut syndrome, migraine. Lacoasamide, Zonisamide, and Eslicarbazepine are indicted in partial epilepsy, tonic-clonic epilepsy, are in phase-III for generalised seizures, in phase-II/II for epilepsy, and neonatal seizures. Ranolazine is used in the treatment of angina pectoris, is in phase-III for acute coronary syndromes, atrial fibrillation, and type 2 diabetes mellitus. Flecainide is used in the treatment of arrhythmia, paroxysmal atrial fibrillation, ventricular arrhythmia, and ventricular tachycardia.
Regional Analysis of Na+ channel Antagonists
Sodium Channel Antagonists Market
Sanofi’s Multaq (Dronedarone) had a total sale of US$ 91 million in Q1 of 2023. Heron Therapeutics's Zynrelef (Bupivacaine/ Meloxicam) had a total sale of US$ 10.196 million in 2022, which was an increase in comparison to the US$ 2,924 sales in 2021. Moreover, currently, Zynrelef is protected by 15 patents in the USA. According to the World Health Organization, around 50 million people worldwide have epilepsy, making it one of the most common neurological diseases globally. Cardiovascular diseases are the leading cause of death globally, accounting for 9,28,741 deaths in 2020 in the USA. According to a research study data, the overall incidence of arrhythmia in COVID-19 patients was 16.8%, where the non-classified arrhythmia had 8.2%, and ventricular fibrillation/ventricular tachycardia had 3.3% incidence rates.
Latin America
Europe
Asia Pacific
Middle East
North America
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Frequently Asked Questions
GTopiramate, Lignocaine, Lacosamide, Ranolazine ER, Phenytoin, Zonisamide are some of the approved Na+ channel antagonists.
Sanofi, AstraZeneca, Gilead Sciences, AbbVie, Heron Therapeutics are some of the major players in the Na+ channel antagonists market.
Major Indications for Na+ channel Antagonists are anaesthesia, postoperative pain, epilepsy, migraine, angina pectoris, atrial fibrillation, ventricular arrhythmia, and ventricular tachycardia.
There are more than 30 molecules in clinical development for Na+ channel antagonists.
- AstraZeneca
- Sanofi
- Gilead
- AbbVie
- Regent Pacific Group
- Boehringer Ingelheim
- Heron Therapeutics
- Gilead Sciences
- Jiangsu Hengrui Pharma
- Allay Therapeutics
- Acasti Pharma
- Sustained Therapeutics