Sodium (Na+) Channel Antagonists Market: Competitive Landscape, Pipeline, and Market Analysis 2023

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.