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Chemical Structure| 2649467-58-1 Chemical Structure| 2649467-58-1
Chemical Structure| 2649467-58-1
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Product Details of Suzetrigine

CAS No. :2649467-58-1
Formula : C21H20F5N3O4
M.W : 473.39
SMILES Code : O=C(N)C1=NC=CC(NC([C@@H]2O[C@](C(F)(F)F)(C)[C@@H](C)[C@H]2C3=CC=C(F)C(F)=C3OC)=O)=C1
Synonyms :
VX-548
MDL No. :N/A

Safety of Suzetrigine

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319
Precautionary Statements:P501-P270-P264-P280-P302+P352-P337+P313-P305+P351+P338-P362+P364-P332+P313-P301+P312+P330

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description Reference
HEK cells expressing human NaV1.8 10 nM 10 minute To assess the inhibition of NaV1.8 by suzetrigine. Results showed that suzetrigine rapidly inhibits NaV1.8 currents. PMID: 39775738
Primary human DRG neurons 1 nM to 10 nM To assess the inhibition of pain signals in human DRG neurons by suzetrigine. Results showed that suzetrigine significantly inhibited action potentials in human DRG neurons. PMID: 39775738
CHO-K1 cells expressing human Nav1.8 1 nM (IC50: 0.27 nM) To assess the inhibition of Nav1.8 channels by VX-548. Results showed that VX-548 potently inhibits Nav1.8 channels with an IC50 of 0.27 nM. PMID: 39322410
Primary human dorsal root ganglia (DRG) neurons 1 nM or 10 nM To assess the inhibition of tetrodotoxin-resistant (NaV1.8) current in primary human DRG neurons. Results showed that VX-548 inhibited NaV1.8 current. PMID: 37530822

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description Reference
Sprague Dawley rats Repeat-dose toxicity model Oral gavage Daily for up to 26 weeks To assess the safety and toxicity of suzetrigine in rats and monkeys. Results showed that suzetrigine was well-tolerated with no significant adverse effects. PMID: 39775738
Cynomolgus monkeys Repeat-dose toxicity model Oral gavage Daily for up to 39 weeks in duration To assess the safety and toxicity of suzetrigine in rats and monkeys. Results showed that suzetrigine was well-tolerated with no significant adverse effects. PMID: 39775738

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT06696443 Diabetic Peripheral Neuropathi... More >>c Pain Less << PHASE3 ENROLLING_BY_INVITATION 2027-01-25 Healthcare Research Network II... More >>, LLC, Flossmoor, Illinois, 60422, United States|MedVadis Research Corporation, Waltham, Massachusetts, 02451, United States|The Center for Clinical Research, Winston-Salem, North Carolina, 27103, United States Less <<
NCT05704556 Pain PHASE1 COMPLETED 2024-03-30 Infigo Clinical Research, DeLa... More >>nd, Florida, 32720, United States|Clinical Pharmacology of Miami, LLC, Miami, Florida, 33014-3616, United States|GCP Research, Saint Petersburg, Florida, 33705, United States|Genesis Clinical Research, Tampa, Florida, 33603, United States|Elixia, Phase 1 Clinical Site, Tampa, Florida, 33618, United States|Southwest Houston Research, Ltd, Houston, Texas, 77099, United States|Clinical Trials of Texas, LLC, San Antonio, Texas, 78229, United States Less <<
NCT05851157 Pain PHASE1 COMPLETED 2023-11-08 ICON Salt Lake City, Salt Lake... More >> City, Utah, 84124, United States Less <<
NCT05560464 Pain PHASE1 COMPLETED 2023-07-24 Division of Clinical Pharmacol... More >>ogy, University of Miami, Miami, Florida, 33136, United States|Orlando Clinical Research Center, Orlando, Oklahoma, 32809, United States Less <<
NCT05661734 Pain PHASE3 COMPLETED 2023-12-12 Anaheim Clinical Trials, Anahe... More >>im, California, 92801, United States|Trovare Clinical Research | Bakersfield, CA, Bakersfield, California, 93301, United States|Mart Medical Research Group LLC, Miami, Florida, 33166, United States|Mart Medical Research Group LLC, South Miami, Florida, 33143, United States|Atlanta Center for Medical Research | Atlanta, GA, Atlanta, Georgia, 30331, United States|Cypress Surgery Center, Wichita, Kansas, 67226, United States|OrthoNebraska Hospital, Omaha, Nebraska, 68144, United States|Center for Orthopaedic Reconstruction and Excellence, Jenks, Oklahoma, 74037, United States|HD Research LLC | First Surgical Hospital, Bellaire, Texas, 77401, United States|HD Research LLC | Legent Orthopedic Hospital, Carrollton, Texas, 75006, United States|Renovatio Clinical, Houston, Texas, 77380, United States|Futuro Clinical Trials, McAllen, Texas, 78501, United States|South Texas Spine & Surgical Hospital, San Antonio, Texas, 78258, United States|Wasatch Clinical Research, Salt Lake City, Utah, 84107, United States Less <<
NCT05455502 Pain PHASE1 COMPLETED 2022-09-17 ICON Salt Lake City, Salt Lake... More >> City, Utah, 84124, United States Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.11mL

0.42mL

0.21mL

10.56mL

2.11mL

1.06mL

21.12mL

4.22mL

2.11mL

References

 

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