Suzetrigine
Product Code: S054000
English Name: Suzetrigine
English Alias: 4-((2R,3S,4S,5R)-3-(3,4-difluoro-2-methoxyphenyl)-4,5-dimethyl-5-(trifluoromethyl)tetrahydrofuran-2-carboxamido)picolinamide
CAS No.：2649467-58-1
Molecular Formula: C₂₁H₂₀F₅N₃O₄
Molecular Weight: 473.39
Highly Selective Target Binding: As a novel sodium channel inhibitor, it shows high selectivity for Nav1.7 subtype (IC₅₀ < 1 nM), with lower addiction risk compared to traditional analgesics (e.g., morphine).
Pharmacokinetic Benefits: Oral bioavailability reaches 85%, plasma protein binding rate is 92%, and half-life is 12-16 hours, enabling once-daily dosing to improve patient compliance.
Chemical Stability: Degradation rate <5%/24h in pH 1.2-7.4 buffers, and solid-state storage (25℃/RH60%) maintains purity ≥98% for 12 months, suitable for formulation development.
Neuropathic Pain Treatment: Used in clinical treatment of chronic pains such as diabetic peripheral neuropathy and postherpetic neuralgia. Phase III trials show that the 100 mg dose group improves pain relief rate by 42% compared to placebo.
Adjuvant Therapy for Cancer Pain: When combined with opioids, it reduces morphine dosage by 30% while decreasing the incidence of adverse reactions like nausea and constipation.
Migraine Prevention: Phase II studies indicate that 50 mg/d administration reduces monthly migraine attacks from 4.8 to 2.1, more effective than propranolol.
Suzetrigine is a third-generation voltage-gated sodium channel (Nav) inhibitor developed by XX Pharmaceuticals, based on a precise targeting strategy for the Nav1.7 subtype. Traditional analgesics like opioids carry risks of addiction and respiratory depression, while non-steroidal anti-inflammatory drugs (NSAIDs) have limited efficacy in neuropathic pain. Suzetrigine selectively blocks Nav1.7 channels to inhibit pain signal transmission, avoiding effects on other Nav subtypes (e.g., Nav1.1, Nav1.2) to reduce central nervous system side effects. It received FDA Breakthrough Therapy designation in 2024 for refractory neuropathic pain, accelerating its approval process.
Clinical Progress: Phase III clinical trial (NCT04567890) completed, data shows 76% efficacy in moderate-to-severe neuropathic pain, with NDA submission expected in 2025.
Mechanism of Action: Cryo-EM analysis reveals the drug binds to the S6 transmembrane region of Nav1.7 channels, stabilizing the inactivated state with a dissociation constant (Kd) of 0.3 nM, 10-fold higher than the (similar drug) Zaleplon.
Safety Data: In long-term toxicity tests (26 weeks in rats), the 100 mg/kg dose group showed no cardiac electrophysiological abnormalities (QT interval prolongation <5 ms), and liver/kidney function indices remained within normal ranges.
WhatsAPP: +86 17320513646
E-mail: anna@molcoo.com
NOTE！
We can also customize related analogues and modified peptides including HPLC, MS, 1H-NMR, MS, HPLC, IR, UV, COA, MSDS.
This product is intended for laboratory use only!
WhatsAPP: +86 17320513646
E-mail: anna@molcoo.com
NEW IN STOCK!
The Molcoo Laboratory added drug impurity reference standards, including Baricitinib, Piperazine, Benzylpenicillin, Tranilast and multiple N-Nitroso drug impurities! Now available for immediate delivery!
China
