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midazolam (ITI 111 / USL 261 / ITI111)

✓ Approved

Ikano Therapeutics · GABRA1 · Small Molecule

What is midazolam?

midazolam is a small molecule developed by Ikano Therapeutics. It is approved for therapeutic indications via inhaled or intranasal.

Drug Profile

Brand NamesITI 111, USL 261, ITI111
CompanyIkano Therapeutics
Drug ClassSmall Molecule
Molecular TargetGABRA1, GABRA2, GABRA3, GABRA4, GABRA5
RouteInhaled, Intranasal
StatusApproved
Sources: ClinicalTrials.gov, Ikano Therapeutics

Mechanism of Action

Molecular Targets

midazolam acts on 5 molecular targets:

GABRA1gamma-aminobutyric acid type A receptor alpha1 subunit (DEE19, ECA4)
GABRA2gamma-aminobutyric acid type A receptor alpha2 subunit (DEE78, EIEE78)
GABRA3gamma-aminobutyric acid type A receptor alpha3 subunit (EPILX2)
GABRA4gamma-aminobutyric acid type A receptor alpha4 subunit ()
GABRA5gamma-aminobutyric acid type A receptor alpha5 subunit (EIEE79, DEE79)
Want deeper analysis?Noah AI can explain complex mechanisms and compare to similar drugs.

Therapeutic Indications

midazolam is developed for 7 unique indications across 2 therapeutic areas.

Therapeutic AreaConditionPhase
Nervous system disordersPartial seizuresPhase III
Nervous system disordersEpilepsyPhase III
Nervous system disordersIdiopathic generalised epilepsyPhase III
Nervous system disordersAmnesiaPhase I
Nervous system disordersAnaesthesiaPhase I

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Related Research Articles

PubMedLaboratory animal research2026-10-15

Faster immobilization and recovery with remimazolam compared to midazolam in medetomidine-butorphanol balanced anesthesia in male Sprague-Dawley rats: a randomized crossover study.

Sasaki Takeru T, Watanabe Masaki M, Nakagawa Ryuya R, Inoue Riyu R et al.

Balanced injectable anesthesia combining an α2-adrenoceptor agonist, a benzodiazepine, and an opioid is widely used in laboratory rodents because it provides sedation, muscle relaxation, and analgesia through complementary pharmacological mechanisms. In Japan, a mixture of medetomidine, midazolam, and butorphanol (MMB) is commonly used as an injectable anesthetic regimen in mice and rats. Remimazolam is an ultra-short-acting benzodiazepine that is rapidly metabolized by tissue esterases and produces no active metabolites. Because of its rapid metabolism and predictable pharmacokinetic profile, remimazolam has attracted attention as a sedative agent in clinical anesthesia and procedural sedation. Replacing midazolam with remimazolam generates a novel balanced anesthetic combination consisting of medetomidine, remimazolam, and butorphanol (MRB). Although this regimen has been investigated in mice, its anesthetic characteristics in rats have not yet been fully evaluated. The present study aimed to compare the anesthetic and physiological effects of MMB and MRB anesthesia in Sprague-Dawley (SD) rats. Both mixtures induced anesthesia in all animals. The MRB regimen produced faster immobilization than the MMB regimen, whereas the time to loss of righting reflex did not differ significantly between regimens. Reflex-based anesthetic depth during the observation period was comparable between the two regimens. Physiological monitoring revealed regimen-dependent differences in time-course dynamics, particularly for oxygen saturation and respiratory rate. For oxygen saturation, pointwise comparisons showed no significant difference after Holm correction, whereas the area under the curve (AUC) analysis did show a significant difference. Linear mixed-effects modeling (LMM) further demonstrated significant group, time, and group × time interaction effects for oxygen saturation, and significant time and group × time interaction effects for respiratory rate. Recovery after atipamezole (ATI) administration was faster in the MRB group, as shown by both return of righting reflex and behavioral recovery score analyses. MRB produced a reflex-score profile comparable to that of MMB while accelerating early immobilization and antagonist-assisted recovery. Substitution of midazolam with remimazolam also altered SpO₂ and respiratory-rate trajectories. MRB may therefore be useful when rapid recovery is desired. However, comparability was limited to the reflex-based scoring system; these findings do not establish equivalence for painful or invasive surgical procedures.

PMID 42875808
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PubMedJournal of anesthesia2026-10-15

Propofol injection discomfort recall after monitored anesthesia care or general anesthesia: a prospective observational cohort study.

Mai Dylan D, Rowshan Kiana K, Modha Dolly D, Chiou Katie K et al.

Pain during propofol injection is common, yet little is known about how often patients remember this experience after anesthesia or which perioperative factors influence memory formation during induction. In this prospective single-center observational cohort study, English-speaking adults (≥ 18 years) receiving propofol under general anesthesia (GA) or monitored anesthesia care (MAC) were enrolled. Perioperative characteristics, intravenous access details, anesthetic medications and clinician-observed injection pain were recorded. On postoperative day 1, patients were interviewed using a standardized questionnaire assessing recall of discomfort during induction. Univariate and multivariate logistic regression analyses calculated adjusted odds ratios (aOR) and identified factors associated with recall. Of the 1,699 enrolled patients, 1,319 completed the postoperative day 1 assessment; 8.1% reported recall of injection discomfort. Multivariate analysis indicated that younger age (aOR = 1.03; 95% CI = 1.01-1.04; p < 0.001), female gender (aOR = 1.69; 95% CI = 1.02-2.82; p = 0.044), hand IV placement (aOR = 2.164; CI 95% = 1.287-3.636; p = 0.004), and absence of midazolam premedication (aOR = 2.62; 95% CI = 1.44-4.78; p = 0.002) were associated with increased recall. Approximately one in twelve patients recalled discomfort during propofol injection. Patient characteristics and modifiable anesthetic practices, particularly premedication and intravenous access site, were associated with memory of propofol injection discomfort. These findings highlight that memory formation during induction represents a distinct and clinically relevant patient-centered outcome.

PMID 42875655
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PubMedJournal of pain and symptom management2026-10-14

Seizure Management in Palliative Care: An Exploratory Cross-sectional Survey of Physician Practices in Germany.

Willert Dr Med Anna-Christin DMA, Ploner Prof Dr Med Christoph J PDMCJ, Gaus Dr Med Verena DMV, Kowski Pd Dr Med Alexander B PDMAB

Seizures pose significant challenges in patients with serious illness, particularly when altered consciousness or dysphagia impair the ability to take antiseizure medication (ASM). However, evidence to inform seizure management in palliative care is limited. Although guidelines exist for epilepsy populations, recommendations for people with serious illness or the end of life are scarce. To characterize seizure management practices and use of ASM in specialized inpatient (SIPC) and outpatient palliative care (SOPC) in Germany. We conducted an exploratory cross-sectional online survey among palliative care physicians in Germany between 08/2023 and 10/2023. The questionnaire covered key domains, including ASM selection, routes of administration, timing and regimens of acute seizure treatment, transition to benzodiazepines (BZD-ASM), ASM discontinuation, and challenges encountered in clinical practice. Among the 111 participating palliative care physicians, 98% reported initiating maintenance ASM, most commonly Levetiracetam (98%) and Midazolam (75%). Most physicians (99%) reported routinely using rescue medication for acute seizures. Midazolam was the most frequently reported first-line rescue medication, preferred in SIPC by 53% and in SOPC by 65%. For second-line treatment of status epilepticus, Levetiracetam was the most frequent choice in SIPC (50%), while Midazolam was preferred in SOPC (52%). Seizure management in palliative care in Germany reflects the specific requirements of patients with serious illness and partly deviates from established epilepsy guidelines. Findings point to a shift towards individualized approaches, including prioritization of BZD-ASM, flexible routes of administration, and increased off-label use. This highlights the need for tailored guidelines and prospective research in palliative care.

PMID 42874890
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PubMedA&A practice2026-10-14

Preoperative Sedation via Cecostomy Tube in an Autistic Adolescent: A Case Report.

Drillings Ian M IM, Jones Stephanie E SE

Preoperative sedation of autistic children is frequently complicated by challenges in communication, sensory processing, and participation in medical care. We report a 40-kg, 13-year-old autistic boy with a preexisting cecostomy tube for chronic constipation, in whom previous oral and intramuscular sedation had failed due to agitation and physical aggression. Midazolam 10 mg (0.25 mg/kg) and ketamine 200 mg (5 mg/kg) were administered via cecostomy tube, producing sedation within 20 minutes. Dental rehabilitation under general anesthesia proceeded uneventfully. Cecal administration of sedatives may be a feasible option when conventional routes are poorly tolerated, although absorption, dosing, and reproducibility remain uncertain.

PMID 42874046
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PubMediScience2026-10-13

Proteomic and functional profiling of suspended jejunal enteroids reveals pharmacokinetic fidelity to native intestine.

Tzioufa Foteini F, Ceylan Merve M, Di Martino Maria Letizia ML, Vo Dinh Son DS et al.

Intestinal enteroids are "mini-guts" that recapitulate essential features of the intestinal epithelium in vitro. We developed and characterized native basal-out (BO) and morphogenically everted apical-out (AO) jejunal enteroids cultured in suspension. Using quantitative proteomics and a range of advanced microscopy techniques, we show that these enteroids progressively adopt protein profiles closely resembling those of freshly isolated villus enterocytes and human jejunal tissue. Optimally differentiated enteroids exhibit mature epithelial morphology, intact barrier function, nutrient absorption, and clinically relevant transporter activity (P-glycoprotein; Pgp/ABCB1, breast cancer resistance protein; BCRP/ABCG2), reflecting in vivo physiology. Metabolic assessment of orally administered cytochrome P450 3A4 (CYP3A4) probe drugs, terfenadine and midazolam, accurately predicted first-pass metabolism and clinical pharmacokinetics via physiologically based pharmacokinetic (PBPK) modeling. These findings establish suspension-grown 3D jejunal enteroids as a translationally relevant, human-derived platform that is advantageous over conventional cell line and animal models for studying drug disposition, nutrient transport, and intestinal barrier function.

PMID 42866664
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PubMedTalanta2026-10-13

Co-assembly SERS strategy for trace detection and intelligent recognition of controlled-drug mixtures.

Bao Lin L, Wang Xiaotian X, Qiu Renna R, He Yingying Y et al.

Surface-enhanced Raman scattering (SERS) is promising for trace chemical analysis, drug detection, and illicit-substance screening. However, conventional assembly-based substrates generally rely on post-assembly soaking, which limits analyte access to nanoscale hot spots and compromises sensitivity and mixture recognition. Here, a co-assembly SERS strategy is proposed by introducing analyte molecules during noble-metal nanoparticle assembly, enabling synchronous enrichment of targets within plasmonic hot-spot regions and enhanced Raman responses. Rhodamine 6G, scarlet and benzimidazole were used as model molecules to verify the superior enhancement of the co-assembly method over the conventional soak mode for cationic, anionic, and drug-like molecules. Sufentanil and midazolam were further selected as representative drug molecules for Raman fingerprint acquisition and low-concentration detection, with lowest tested concentrations of 5 ppm and 0.5 ppm, respectively. To address peak overlap, intensity fluctuation and manual interpretation challenges in mixed-drug spectra, a rule-based multidimensional spectral matching algorithm was developed by integrating peak-position, peak-intensity-ratio and local waveform-similarity matching through confidence-score fusion. This work provides a proof-of-concept for combining co-assembly-enhanced SERS with rule-based multidimensional spectral matching for the recognition of representative controlled-drug molecules in model mixtures.

PMID 42863173
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