cyclobenzaprine
Small molecule targets HTR2A, HTR2C via inhibition
Regulatory milestones approvals, filings & regulatory actions · 2 recorded
| Milestone | Jurisdiction | Brand | Indication | Date | Sentence it was read from |
|---|---|---|---|---|---|
| Label expansion | US (FDA) | FLEXERIL | — | 2003-02-03 | fda.gov ↗ |
| Approved | US (FDA) | FLEXERIL | — | 1977-08-26 | fda.gov ↗ |
Trials 36 · a red edge is where a trial was stopped
| Phase | Registry id | Dates | Indication | Sponsor | Status | Outcome |
|---|---|---|---|---|---|---|
| Phase 19 trials | ||||||
| Phase 1 | NCT07413367 | Dec 2025 → Feb 2026 overdue | — | Tonix Pharmaceuticals, Inc. | Active not recruiting | No outcome recorded |
| Phase 1 | NCT07464535 | Mar → Apr 2022 | — | Tonix Pharmaceuticals, Inc. | Completed | No outcome recorded |
| Phase 1 | NCT04164719 | Oct → Dec 2019 | — | Tonix Pharmaceuticals, Inc. | Completed | No outcome recorded |
| Phase 1 | NCT03443960 | Jan → Apr 2018 | — | Tonix Pharmaceuticals, Inc. | Completed | No outcome recorded |
| Phase 1 | NCT03353922 | Jul → Dec 2017 | — | Neurana Pharmaceuticals, Inc. | Completed | No outcome recorded |
| Phase 1 | NCT01689259 | Sep 2012 → Dec 2013 | — | Tonix Pharmaceuticals, Inc. | Completed | No outcome recorded |
| Phase 1 | NCT01634412 | Jun 2012 → Sep 2013 | — | Tonix Pharmaceuticals, Inc. | Completed | No outcome recorded |
| Phase 1 | NCT01490788 | Nov → Dec 2011 | — | Tonix Pharmaceuticals, Inc. | Completed | No outcome recorded |
| Phase 1 | NCT00913419 | Nov → Dec 1988 | depressive disorder | Sandoz | Completed | No outcome recorded |
| Phase 26 trials | ||||||
| Phase 2 | NCT07621237 | Jun 2026 → Feb 2028 expected | major depressive disorder | Tonix Pharmaceuticals, Inc. | Recruiting | No outcome recorded |
| Phase 2 | NCT06636786 | Mar 2025 → Sep 2026 expected | acute stress disorder, cognitive disorder, post-traumatic stress disorder | University of North Carolina, Chapel Hill | Recruiting | No outcome recorded |
| Phase 2 | NCT05372887 | Oct → Nov 2022 | post-traumatic stress disorder | Tonix Pharmaceuticals, Inc. | Withdrawn | No outcome recorded |
| Phase 2 | NCT05472090 | Aug 2022 → Jul 2023 | COVID-19, long COVID-19 | Tonix Pharmaceuticals, Inc. | Completed | No outcome recorded |
| Phase 2 | NCT02421679 | Apr 2015 → May 2016 | post-traumatic stress disorder | Tonix Pharmaceuticals, Inc. | Completed | No outcome recorded |
| Phase 2 | NCT01921296 | Aug 2013 → May 2014 | sleep disorder, initiating and maintaining sleep | Lynn Henry | Terminated | No outcome recorded |
| Phase 2/32 trials | ||||||
| Phase 2/3 | NCT07404397 | Feb → Dec 2026 expected | anismus | University of Michigan | Recruiting | No outcome recorded |
| Phase 2/3 | NCT01903265 | Sep 2013 → Jul 2014 | fibromyalgia | Tonix Pharmaceuticals, Inc. | Completed | No outcome recorded |
| Phase 314 trials | ||||||
| Phase 3 | NCT05683574 | May 2026 → Oct 2027 | — | Eurofarma Laboratorios S.A. | Withdrawn | No outcome recorded |
| Phase 3 | NCT05273749 | Apr 2022 → Nov 2023 | fibromyalgia | Tonix Pharmaceuticals, Inc. | Completed | No outcome recorded |
| Phase 3 | NCT04508621 | Jul 2020 → Nov 2021 | fibromyalgia | Tonix Pharmaceuticals, Inc. | Completed | No outcome recorded |
| Phase 3 | NCT04172831 | Dec 2019 → Oct 2020 | fibromyalgia | Tonix Pharmaceuticals, Inc. | Completed | No outcome recorded |
| Phase 3 | NCT03841773 | Mar 2019 → Apr 2020 | post-traumatic stress disorder | Tonix Pharmaceuticals, Inc. | Terminated | No outcome recorded |
| Phase 3 | NCT03508700 | Apr 2018 → Sep 2019 | post-traumatic stress disorder | Tonix Pharmaceuticals, Inc. | Completed | No outcome recorded |
| Phase 3 | NCT03110575 | Jun 2017 → Jul 2018 | post-traumatic stress disorder | Tonix Pharmaceuticals, Inc. | Terminated | No outcome recorded |
| Phase 3 | NCT03062540 | Mar 2017 → Jul 2018 | post-traumatic stress disorder | Tonix Pharmaceuticals, Inc. | Terminated | No outcome recorded |
| Phase 3 | NCT02814565 | Oct 2016 → Feb 2017 | — | Takeda | Completed | No outcome recorded |
| Phase 3 | NCT02829814 | Jul → Sep 2016 | fibromyalgia, myofascial pain syndrome, neuromuscular disease, rheumatic disorder | Tonix Pharmaceuticals, Inc. | Terminated | No outcome recorded |
| Phase 3 | NCT02589275 | Aug 2015 → Sep 2016 | fibromyalgia | Tonix Pharmaceuticals, Inc. | Completed | No outcome recorded |
| Phase 3 | NCT02436096 | Apr 2015 → Sep 2016 | fibromyalgia, myofascial pain syndrome, neuromuscular disease, rheumatic disorder | Tonix Pharmaceuticals, Inc. | Completed | No outcome recorded |
| Phase 3 | NCT02015234 | Dec 2013 → Aug 2015 | fibromyalgia | Tonix Pharmaceuticals, Inc. | Completed | No outcome recorded |
| Phase 3 | NCT01421433 | May → Aug 2012 | — | Farmoquimica S.A. | Unknown | No outcome recorded |
| Phase 43 trials | ||||||
| Phase 4 | NCT07664956 | Jul → Sep 2026 expected | adenomyosis, chronic pain syndrome, endometriosis, endometritis +2 | Christiana Care Health Services | Not yet recruiting | No outcome recorded |
| Phase 4 | NCT01041495 | Jun 2009 → Mar 2013 | fibromyalgia | State University of New York - Upstate Medical University | Terminated | No outcome recorded |
| Phase 4 | NCT00246389 | ? → Jul 2004 | — | McNeil Consumer & Specialty Pharmaceuticals, a Division of McNeil-PPC, Inc. | Completed | No outcome recorded |
| Phase not applicable2 trials | ||||||
| — | NCT01081990 | Apr 2010 → Jul 2014 | — | Endeavor Health | Completed | No outcome recorded |
| — | NCT00635037 | Jun 2004 → Feb 2005 | myofascial pain syndrome | Federal University of São Paulo | Completed | No outcome recorded |
Also used as a comparator or background therapy in 17 trials
| Phase | Registry id | Dates | Indication | Sponsor | Status | Outcome |
|---|---|---|---|---|---|---|
| Phase 12 trials | ||||||
| Phase 1 | NCT04407377 Comparator | Jun → Oct 2020 | — | Neurana Pharmaceuticals, Inc. | Completed | No outcome recorded |
| Phase 1 | NCT01889173 Comparator | Jun → Dec 2013 | — | Tonix Pharmaceuticals, Inc. | Completed | No outcome recorded |
| Phase 22 trials | ||||||
| Phase 2 | NCT02277704 Comparator | Oct 2014 → May 2016 | post-traumatic stress disorder | Tonix Pharmaceuticals, Inc. | Completed | No outcome recorded |
| Phase 2 | NCT00790270 Comparator | Jan 2003 → Jan 2004 | — | Stony Brook University | Completed | No outcome recorded |
| Phase 36 trials | ||||||
| Phase 3 | NCT03127592 Comparator | Oct 2020 → Jul 2022 | — | Apsen Farmaceutica S.A. | Terminated | No outcome recorded |
| Phase 3 | NCT02642861 Comparator | Oct 2018 → Dec 2019 | cirrhosis of liver | Tanta University | Unknown | No outcome recorded |
| Phase 3 | NCT03025113 Comparator | Mar 2018 → Nov 2019 | musculoskeletal system disorder | EMS | Completed | No outcome recorded |
| Phase 3 | NCT02862977 Comparator | Nov 2017 → Jun 2019 | musculoskeletal system disorder | EMS | Completed | No outcome recorded |
| Phase 3 | NCT01587508 Comparator | May 2013 | — | Eurofarma Laboratorios S.A. | Withdrawn | No outcome recorded |
| Phase 3 | NCT01151787 Comparator | Jul 2010 → Sep 2013 | migraine disorder | Kennedy Medical Group | Terminated | No outcome recorded |
| Phase 44 trials | ||||||
| Phase 4 | NCT04990804 Background | Aug 2021 → Feb 2022 | spinal cord disorder, substance-related disorder | Vanderbilt University Medical Center | Terminated | No outcome recorded |
| Phase 4 | NCT04240626 Background | Jan 2021 → Jun 2026 overdue | morbid obesity | University of California, Davis | Active not recruiting | No outcome recorded |
| Phase 4 | NCT04704297 Comparator | Dec 2020 → Jul 2022 overdue | myofascial pain syndrome | Madigan Army Medical Center | Recruiting | No outcome recorded |
| Phase 4 | NCT01587274 Comparator | Apr 2012 → Oct 2014 | — | Montefiore Medical Center | Completed | No outcome recorded |
| Phase not applicable3 trials | ||||||
| — | NCT03119324 Comparator | Sep 2015 → Jun 2016 | temporomandibular joint disorder | University of Roma La Sapienza | Completed | No outcome recorded |
| — | NCT02974166 Background | Mar 2012 → Nov 2015 | temporomandibular joint disorder | Instituto Brasileiro de Osteopatia | Completed | No outcome recorded |
| — | NCT01028014 Comparator | Apr 2010 → Apr 2011 | urethral disorder | University of Alabama at Birmingham | Completed | No outcome recorded |
Evidence & citations 21 cited values
Every value below carries the sentence it was read from. 55 sources stand behind the page.
| Field | Value | Cited text |
|---|---|---|
| Known as | cyclobenzaprine | “The use of low-dose sublingual formulation of cyclobenzaprine (TNX-102 SL) dosed nightly for fibromyalgia is supported by the results of TNX-CY-F202 Phase 2b study -- the...” NCT02829814 ↗38“TNX-102 SL is a bedtime sublingual formulation of cyclobenzaprine with potent binding and antagonist activity at 5-HT2A, α1-adrenergic, H1 histaminergic, and M1 muscarinic...” PMID 38350291 ↗ Feb 2024 “This 12-week randomized multicenter trial evaluated efficacy and safety of TNX-102 SL, a bedtime sublingual formulation of cyclobenzaprine, in patients with military-related...” PMID 33979763 ↗ Apr 2021 “This is a 12-week, multicenter, randomized, double-blind, placebo-controlled, fixed-dose study that will investigate the efficacy and safety of 5.6 mg TNX-102 SL (2 x 2.8 mg...” NCT05372887 ↗ “OBJECTIVE: To evaluate the efficacy and safety of TNX-102 SL, a once-nightly sublingual formulation of cyclobenzaprine, in reducing pain in patients with fibromyalgia (FM).” PMID 37165930 ↗ Jul 2023 “sublingual TNX-102 2.4 mg (a new formulation of cyclobenzaprine designed to result in increased dosage precision and decreased potential for morning grogginess)” NCT01634412 ↗ “TNX-102 2.4 mg SL Tablets (a new formulation of cyclobenzaprine designed to result in increased dosage precision and decreased potential for morning grogginess)” NCT01689259 ↗ “We evaluated efficacy and safety of bedtime TNX-102 SL (sublingual cyclobenzaprine) 5.6 mg for treatment of fibromyalgia.” PMID 40627411 ↗ Jan 2026 “Dolamin Flex (lysine clonixinate and cyclobenzaprine). Tablets, administered 3 times a day, for 7 consecutive days.” NCT01421433 ↗ “Cyclobenzaprine HCl sublingual tablets. The tablets are yellow, round, and biconvex with a "T" debossed on one face” NCT07464535 ↗ “2 x TNX-102 SL (cyclobenzaprine HCl sublingual tablets) 2.8 mg once daily for 20 consecutive days” NCT03443960 ↗ “a study drug called TNX-102 SL [cyclobenzaprine hydrochloride (HCl) sublingual (SL) tablets]” NCT07413367 ↗ “TNX-102 SL 5.6 mg (2 x 2.8 mg tablets) - a sublingual formulation of cyclobenzaprine” NCT03841773 ↗ “one 5 days cycle of cyclobenzaprine hydrochloride (10 mg a day)” NCT03119324 ↗ “Cyclobenzaprine 5 mg, 1 tablet once under fasting conditions” NCT01490788 ↗ “10 mg/day cyclobenzaprine and 500 mg dipyrone every 8 h” NCT00635037 ↗ “Methocarbamol 750mg BID or Cyclobenzaprine 5-10 mg TID” NCT04990804 ↗ “Low dose cyclobenzaprine sublingual tablets” NCT02436096 ↗ “10 mg of cyclobenzaprine nightly by mouth” NCT04704297 ↗ “cyclobenzaprine HCl sublingual tablets” NCT03508700 ↗ |
| Known as | AMRIX | “AMRIX® (cyclobenzaprine HCl ER Capsules) 30 mg” NCT03443960 ↗ |
| Known as | Ciclobenzaprina | ChEMBL registry synonym — accepted as the source's own label CHEMBL669 ↗ |
| Known as | cyclobenzaprine HCl | “Cyclobenzaprine HCl sublingual tablets. The tablets are yellow, round, and biconvex with a "T" debossed on one face” NCT07464535 ↗4“Cyclobenzaprine HCl Tablets 10 mg, Cord Laboratories” NCT00913419 ↗ “cyclobenzaprine HCl sublingual tablets” NCT03508700 ↗ |
| Known as | Cyclobenzaprine Hydrochloride | “a study drug called TNX-102 SL [cyclobenzaprine hydrochloride (HCl) sublingual (SL) tablets]” NCT07413367 ↗5“one 5 days cycle of cyclobenzaprine hydrochloride (10 mg a day)” NCT03119324 ↗ “cyclobenzaprine hydrochloride 15 mg capsule (XL - Mitrul®)” NCT05683574 ↗ “Drug: Cyclobenzaprine Hydrochloride 10 MG” NCT04407377 ↗ |
| Known as | cyclobenzaprine hydrochloride is Amrix 15mg/daily | “cyclobenzaprine hydrochloride is Amrix 15mg/daily” NCT01151787 ↗ |
| Known as | Flexeril | “Cyclobenzaprine, aka Flexeril®, is NOT an experimental drug and is already approved by the Food and Drug Administration (FDA) for acute, painful muscle spasms.” NCT07664956 ↗2“Cyclobenzaprine (Flexeril®) in conjunction with NSAIDs has long been the basis for management of acute musculoskeletal injuries” NCT01081990 ↗ |
| Known as | Miosan | “cyclobenzaprine - Miosan®” NCT01587508 ↗ |
| Known as | MK-130 (AS THE BASE) | ChEMBL registry synonym — accepted as the source's own label CHEMBL669 ↗ |
| Known as | MK-130 HYDROCHLORIDE | ChEMBL registry synonym — accepted as the source's own label CHEMBL669 ↗ |
| Known as | NSC-169900 | ChEMBL registry synonym — accepted as the source's own label CHEMBL669 ↗ |
| Known as | NSC-173379 | ChEMBL registry synonym — accepted as the source's own label CHEMBL669 ↗ |
| Known as | NSC-78206 | ChEMBL registry synonym — accepted as the source's own label CHEMBL669 ↗ |
| Known as | TNX-102 | “TNX-102 2.4 mg SL Tablets (a new formulation of cyclobenzaprine designed to result in increased dosage precision and decreased potential for morning grogginess)” NCT01689259 ↗ |
| Known as | TNX-102 SL | “The use of low-dose sublingual formulation of cyclobenzaprine (TNX-102 SL) dosed nightly for fibromyalgia is supported by the results of TNX-CY-F202 Phase 2b study -- the...” NCT02829814 ↗17“TNX-102 SL is a bedtime sublingual formulation of cyclobenzaprine with potent binding and antagonist activity at 5-HT2A, α1-adrenergic, H1 histaminergic, and M1 muscarinic...” PMID 38350291 ↗ Feb 2024 “This 12-week randomized multicenter trial evaluated efficacy and safety of TNX-102 SL, a bedtime sublingual formulation of cyclobenzaprine, in patients with military-related...” PMID 33979763 ↗ Apr 2021 “This is a 12-week, multicenter, randomized, double-blind, placebo-controlled, fixed-dose study that will investigate the efficacy and safety of 5.6 mg TNX-102 SL (2 x 2.8 mg...” NCT05372887 ↗ “OBJECTIVE: To evaluate the efficacy and safety of TNX-102 SL, a once-nightly sublingual formulation of cyclobenzaprine, in reducing pain in patients with fibromyalgia (FM).” PMID 37165930 ↗ Jul 2023 “TNX-102 SL (cyclobenzaprine HCl sublingual tablets) taken sublingually (under the tongue) in the ED and each day at bedtime for a total of 2 weeks.” NCT06636786 ↗ “2 x TNX-102 SL (cyclobenzaprine HCl sublingual tablets) 2.8 mg once daily for 20 consecutive days” NCT03443960 ↗ “TNX-102 SL 5.6 mg (2 x 2.8 mg tablets) - a sublingual formulation of cyclobenzaprine” NCT03841773 ↗ |
| Known as | XL - Mitrul | “cyclobenzaprine hydrochloride 15 mg capsule (XL - Mitrul®)” NCT05683574 ↗ |
| Action | Inhibit | “potent binding and antagonist activity at 5-HT2A, α1-adrenergic, H1 histaminergic, and M1 muscarinic receptors” PMID 38350291 ↗ Feb 20242“Serotonin 2c (5-HT2c) receptor antagonist” CHEMBL669 ↗ “Serotonin 2a (5-HT2a) receptor antagonist” CHEMBL669 ↗ |
| Modality | Small molecule | — CHEMBL669 ↗ |
| Route | Oral | “Patients receive cyclobenzaprine HCl 5 mg administered orally three times a day for one week” NCT00246389 ↗ |
| Target | HTR2A | “Serotonin 2a (5-HT2a) receptor antagonist” CHEMBL669 ↗ |
| Target | HTR2C | “Serotonin 2c (5-HT2c) receptor antagonist” CHEMBL669 ↗ |