Drug Database
BA

baclofen (Ozobax)

✓ Approved

Metacel Pharmaceuticals · GABBR1 · Small Molecule

What is baclofen?

baclofen is a small molecule developed by Metacel Pharmaceuticals. It is approved for therapeutic indications via oral (po).

Drug Profile

Brand NamesOzobax
CompanyMetacel Pharmaceuticals
Drug ClassSmall Molecule
Molecular TargetGABBR1
RouteOral (PO)
StatusApproved
Sources: ClinicalTrials.gov, Metacel Pharmaceuticals

Mechanism of Action

Molecular Targets

baclofen acts on 1 molecular target:

GABBR1gamma-aminobutyric acid type B receptor subunit 1 (GABABR1, GB1)
Want deeper analysis?Noah AI can explain complex mechanisms and compare to similar drugs.

Therapeutic Indications

baclofen is developed for 1 unique indication across 1 therapeutic area.

Therapeutic AreaConditionPhase
Nervous system disordersMuscle spasticity✓ Approved

Related Research Articles

PubMedJournal of microencapsulation2026-07-17

In vitro and in vivo investigation for nose to brain delivery of surface modified PLGA nanoparticles of baclofen.

Rai Garima G, Sharma Surbhi S, Devtalla Harshit H, Gauba Pammi P et al.

Baclofen is widely used for neuropathic pain but has limited therapeutic efficacy due to poor brain bioavailability and restricted penetration across the blood-brain barrier. To develop and evaluate polysorbate 80-coated PLGA nanoparticles for enhanced brain delivery of baclofen. Baclofen-loaded PLGA nanoparticles were prepared using the double emulsification solvent evaporation method and characterized for particle size, polydispersity index, zeta potential, entrapment efficiency, and drug loading. In vitro drug release, cytotoxicity, cellular uptake, and in vivo biodistribution studies were performed. The optimized nanoparticles showed a mean particle size of 141.2 nm, entrapment efficiency of 90.2%, and drug loading of 10.4%. Sustained drug release (79.42% over 48 h), minimal neuronal cytotoxicity, and enhanced cellular uptake were observed. In vivo biodistribution studies demonstrated significantly higher brain accumulation of baclofen compared with conventional delivery. Polysorbate 80-coated PLGA nanoparticles effectively enhanced baclofen brain delivery, providing sustained release, good biocompatibility, and improved brain targeting, indicating their potential for more effective neuropathic pain management.

PMID 42464757
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PubMedClinical practice and cases in emergency medicine2026-07-16

A Case Report of Delayed, Severe, Paroxysmal Muscle Cramping After Chilean Rose Tarantula (Grammostola rosea) Envenomation.

Gooley Brian B, Hughes Kirk K, Gooley Mark M, Keyler Daniel D et al.

Grammostola rosea (Chilean rose tarantula) is a common exotic pet belonging to the Theraphosidae (tarantula) family. Case reports of theraphosid bites in adults commonly describe local tissue damage and local pain. Muscle spasms have also been described as a result of the bites but are rarer. We present a case of severe and persistent muscle spasms after a G rosea bite, which is uncommonly reported in the literature. A 42-year-old woman was holding a G rosea tarantula when she was bit on the forearm. Within hours, severe local muscle cramping occurred. Due to worsening cramping, she initially presented to the emergency department the day after the bite, and again on the following day. She was admitted on her second visit and treated with diazepam, cephalexin, diphenhydramine, baclofen, cefpodoxime, doxycycline, prednisone, and topical hydrocortisone. Her laboratory testing was unremarkable, and while medical management may have mildly improved her symptoms, painful cramping persisted. After discharge, her paroxysmal muscle cramping continued for four weeks before completely resolving. While local tissue damage and pain are common, G rosea bites may lead to severe muscle cramping that persists for weeks. Standard laboratory testing may be completely normal in these cases. Muscle cramps may be persistent and are difficult to manage.

PMID 42456293
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PubMedCase reports in anesthesiology2026-07-12

Perioperative Pregabalin for Recurrent Intractable Hiccups: A Case Report and Literature Review.

Lei David D, Yamaguchi Craig T L CTL, Moody Alastair E AE, Swenson Jeffrey D JD

Involuntary diaphragmatic spasms, "hiccups," commonly resolve spontaneously over a few minutes but can occasionally persist, presenting a challenging perioperative problem. Pregabalin is a frequently utilized gabapentinoid in the treatment of neuropathic pain, but its effectiveness for treating hiccups during the perioperative period has not been well established. We present a patient with a 7-year history of intractable hiccups resistant to chlorpromazine, baclofen, gabapentin, and cervical epidural injections presenting for orthopedic surgery. Perioperative and postoperative pregabalin administration significantly reduced the frequency and severity of hiccups. This case demonstrates the potential for pregabalin in the management of refractory hiccups.

PMID 42436812
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PubMedChild's nervous system : ChNS : official journal of the International Society for Pediatric Neurosurgery2026-07-09

Stepwise surgical management of spasticity and dystonia in severe pediatric cerebral palsy: a case report involving selective dorsal rhizotomy, intrathecal baclofen therapy, and deep brain stimulation.

Byun Jong Won JW, Lee Jae Meen JM, Shin Yong Beom YB, Yoon Jin A JA et al.

Children with severe cerebral palsy often encounter significant challenges due to refractory spasticity and dystonia in their upper and lower limbs, which are unresponsive to pharmacological treatments. Selecting appropriate surgical interventions is essential for effective management of these severe symptoms. We present the case of a 10-year-old child with severe cerebral palsy who experienced intractable spasticity in both upper and lower limbs that was not controlled by medication. Weighing less than 20 kg, the child initially underwent selective dorsal rhizotomy (SDR), which significantly reduced lower limb spasticity and contributed to an increase in body weight. Approximately 1 year later, to address persistent upper limb spasticity, intrathecal baclofen therapy (ITB) was administered, resulting in a marked improvement in spasticity and quality of life. However, nocturnal dystonia continued to disrupt sleep. As a result, 2 years after ITB, deep brain stimulation (DBS) was performed, leading to substantial relief from both spasticity and dystonia and further enhancing the child's overall well-being. In cases of severe cerebral palsy, a sequential, symptom-targeted surgical approach can be highly beneficial. Implementing a strategy that includes multiple interventions tailored to the patient's evolving clinical needs can significantly improve outcomes and quality of life.

PMID 42420630
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PubMedStereotactic and functional neurosurgery2026-07-09

Global Research Trends in the Surgical Management of Spasticity: A Systematic Review and Bibliometric Analysis.

Mantovani Giorgio G, Dauleac Corentin C, Cavallo Michele Alessandro MA, Mertens Patrick P

Surgical interventions remain a cornerstone in the multidisciplinary management of spasticity. While historically centered on pediatric cerebral palsy, the field has expanded with emerging techniques and shifting epidemiological patterns. Despite this evolution, no bibliometric study has analyzed the scientific landscape of surgical spasticity treatment. This study provides a comprehensive bibliometric analysis of global research trends, identifying historical milestones, emerging techniques, and leading institutions. A systematic search of the Scopus database was conducted using a tailored query to retrieve English‑language articles on surgical interventions for spasticity. Data were analyzed using bibliometric software to assess publication trends, citation metrics, keyword evolution, and network relationships among authors, institutions, and countries. A total of 1049 articles published between 1980 and 2024 were included. The most cited works focused on intrathecal baclofen therapy and selective dorsal rhizotomy. Recent years show growing interest in peripheral procedures such as selective neurotomies and nerve transfers, while central techniques such as DREZotomy and deep brain stimulation display declining trends. Although most publications target pediatric populations, studies involving adult patients are increasing, reflecting the rise of acquired spasticity. Most articles were published in high‑impact journals, yet randomized controlled trials remain scarce. This study highlights a progressive shift toward more tailored, peripheral, and neuromodulatory approaches, particularly in adult care. Future research should prioritize comparative trials and the integration of combined neuro‑orthopedic strategies, supported by international collaboration and methodological standardization.

PMID 42424247
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PubMedBiochemical pharmacology2026-07-08

Activation of GABABR alleviates colitis by reprogramming macrophage polarization via the IRAK-M/NLRP3/NF-κB pathway.

Xie Haoxian H, Liu Huilin H, Xiu Yixin Y, Lao Rongkang R et al.

Although the metabotropic GABA type B receptor (GABABR) has emerged as an immune modulator, its specific role in regulating the dysregulated macrophage polarization that drives inflammatory bowel disease (IBD) pathogenesis remains undefined. Utilizing a dextran sulfate sodium-induced colitis model and lipopolysaccharide-stimulated macrophages, we observed that colonic inflammation significantly downregulates GABABR expression concomitant with a pronounced shift toward M1 polarization. Pharmacological activation of GABABR with baclofen ameliorated clinical and histopathological manifestations, restored mucosal barrier integrity, and suppressed mast cell accumulation. Mechanistically, baclofen upregulated the negative regulator Interleukin-1 receptor-associated kinase M (IRAK-M), which inhibited the NOD-like receptor family pyrin domain containing 3 (NLRP3) / nuclear factor-kappa B (NF-κB) signaling cascade and promoted repolarization toward the protective M2 phenotype. The essential role of IRAK-M was confirmed via genetic knockout; such ablation abolished the protective effects of baclofen, exacerbated colitis, enhanced NLRP3/NF-κB activation, and drove M1 polarization. Transcriptomic analysis of IRAK-M-deficient mice revealed profound alterations in immune-related pathways, validating IRAK-M as a critical downstream effector. Furthermore, inhibition of NLRP3 with CY-09 and genetic deletion recapitulated the M2-promoting effects observed with GABABR activation. Collectively, these findings establish GABABR as a pivotal regulator of intestinal immune homeostasis that controls macrophage polarization through the IRAK-M/NLRP3/NF-κB axis, positioning GABABR as a promising therapeutic target for IBD.

PMID 42413737
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