Drug Database
ZO

zolpidem tartrate (Intermezzo / zolpidem, TransOral)

✓ Approved

Transcept Pharmaceuticals · GABRA1 · Small Molecule

What is zolpidem tartrate?

zolpidem tartrate is a small molecule developed by Transcept Pharmaceuticals. It is approved for therapeutic indications via oral (po) or sublingual (sl)/oral transmucosal.

Drug Profile

Brand NamesIntermezzo, zolpidem, TransOral
CompanyTranscept Pharmaceuticals
Drug ClassSmall Molecule
Molecular TargetGABRA1
RouteOral (PO), Sublingual (SL)/Oral Transmucosal
StatusApproved
Sources: ClinicalTrials.gov, Transcept Pharmaceuticals

Mechanism of Action

Molecular Targets

zolpidem tartrate acts on 1 molecular target:

GABRA1gamma-aminobutyric acid type A receptor alpha1 subunit (DEE19, ECA4)
Want deeper analysis?Noah AI can explain complex mechanisms and compare to similar drugs.

Therapeutic Indications

zolpidem tartrate is developed for 1 unique indication across 1 therapeutic area.

Therapeutic AreaConditionPhase
Psychiatric disordersInsomnia✓ Approved

Related Research Articles

PubMedJournal of materials science. Materials in medicine2026-05-24

Synergistic effects of denosumab and BMP-2 on bone regeneration in critical-sized femoral defects in ovariectomized rats.

Tao ZhouShan Z, Cheng WenJing W, Wang Lin L, Qi Wei W

Osteoporotic bone defects pose significant clinical challenges due to poor natural repair capacity. Denosumab (DNB) strongly inhibits osteoclast activity, while Bone morphogenetic protein-2 (BMP-2) effectively promotes bone formation; however, it remains unclear whether combining DNB and BMP-2 can enhance bone repair in estrogen deficiency-induced osteoporosis. We investigated the effects of local BMP-2 implantation and systemic DNB treatment on bone regeneration in ovariectomized (OVX) rats. Micro-computed tomography(Micro-CT) and H&E staining showed that DNB and BMP-2 synergistically accelerated healing of osteoporotic bone defects over 12 weeks. Immunofluorescence, immunohistochemistry, and biomechanical analyses revealed that DNB/BMP-2 increased expression of osteopontin(OPN), osteoclastogenesis inhibitory factor(OPG) and Runt-related transcription factor 2 (RUNX2), and decreased tartrate-resistant acid phosphatase (TRAP) and Tumor Necrosis Factor-α (TNF-α) levels compared to the OVX group (all P < 0.05). Moreover, DNB/BMP-2 significantly improved torsional stiffness and maximum compressive force versus either treatment alone (all P < 0.05). The findings demonstrate that systemic DNB combined with local BMP-2 rapidly promotes femoral metaphyseal bone regeneration in osteoporotic rats.

PMID 42176116
Read full article →
PubMedPharmacology, biochemistry, and behavior2026-05-23

Discriminative stimulus and locomotor activity profiles of nicotine and varenicline.

Kusi-Boadum Nana Kofi NK, Taylor Cynthia M CM, Shetty Ritu A RA, Sumien Nathalie N et al.

These studies characterized the locomotor and discriminative stimulus effect of nicotine, mecamylamine, and varenicline in efforts to optimize detection of substitutes and antagonists of nicotine. We compared nicotine- and varenicline-induced LMA to confirm the assay's utility as a predictor of therapeutic potential, and determined how training dose and pretreatment interval affect the nicotine discriminative stimulus, and influence varenicline's ability to substitute. Mice were assessed for LMA following injection of nicotine tartrate (NicT), varenicline, mecamylamine, or saline. A time-course study in rats was conducted to identify the minimum effective dose and shortest pretreatment time at which NicT exerts discriminative stimulus control. Cohorts were trained using (i) a standard 0.4 mg/kg, 15-min, (ii) a 0.1 mg/kg, 5-min, or (iii) a dose-fading (0.4 → 0.1 mg/kg), 5-min protocols. Substitution and antagonism tests were conducted with varenicline and mecamylamine. Nicotine and varenicline produced early depressant and delayed stimulant effects; mecamylamine was inactive. Nicotine's depressant effect had four-fold greater potency than varenicline. In discrimination, 0.1 mg/kg NicT fully substituted at a 5-min pretreatment interval. The low-dose and faded groups showed enhanced sensitivity. Varenicline fully substituted in the standard and faded groups but only partially in the low-dose group. The matching biphasic profiles of nicotine and varenicline suggest that LMA studies may be useful in identifying compounds with therapeutic potential targeting the nicotinic acetylcholine receptor. Low-dose, short pre-treatment time discrimination procedures reveal varenicline's predicted α4β2 partial agonist profile, whereas high dose, long pre-treatment times may broaden the nicotine cue and mask partial substitution.

PMID 42173370
Read full article →
PubMedOrganic & biomolecular chemistry2026-05-22

One-step synthesis of Zolpidem and its analogues via visible light induced coupling of imidazo[1,2-α]pyridines with 2-bromoacetamides.

Zhang Shiyu S, Li Min M, Xiao Yuanjiu Y, Zhang Yangjianyun Y et al.

A novel and efficient strategy for synthesizing the drug Zolpidem and its analogues via the coupling of imidazo[1,2-α]pyridines with 2-bromoacetamides under blue LED irradiation has been developed. Starting from two commercially available intermediates, Zolpidem can be synthesized in just one single step. Additionally, the reaction is carried out at 25 °C without the need for any transition metal catalyst or photocatalyst and is very simple to run. Compared with conventional Zolpidem synthesis, this new method features high efficiency, operational simplicity and excellent atom and step economy. These notable features make this protocol highly attractive for possible industrial applications.

PMID 42171050
Read full article →
PubMedTranslational breast cancer research : a journal focusing on translational research in breast cancer2026-05-22

The efficacy and safety of metronomic vinorelbine combined with anlotinib in HER2-negative advanced breast cancer: a prospective, single-arm clinical study.

Wang Xinli X, Yang Ting T, Zhang Junmei J, Yang Jin J et al.

In the era of chronic cancer management, second-line treatment for HER2-negative (HER2-) advanced breast cancer demands convenient and safe therapeutic options. Vinorelbine tartrate soft capsules are an oral chemotherapeutic agent, and anlotinib is an oral multi-target anti-angiogenic drug. The aim of this study is to investigate the efficacy and safety of metronomic vinorelbine combined with anlotinib in HER2- advanced breast cancer. This is a prospective, single-arm, single center clinical study. Women with metastatic HER- breast cancer who had received one prior line of endocrine ± targeted therapy or chemotherapy ± immunotherapy were enrolled. Treatment consisted of vinorelbine tartrate soft capsules 30-50 mg orally three times weekly (every other day) plus anlotinib 12 mg once daily on days 1-14 of each 21-day cycle. The primary endpoint was progression-free survival (PFS); secondary endpoints included objective response rate (ORR), disease control rate (DCR), and adverse events (AEs). Fifty-eight patients were enrolled. ORR was 63.8% and DCR 89.7%. Median PFS (mPFS) was 7.0 months [95% confidence interval (CI): 6.4-7.8]. Subgroup analyses showed that patients with prior PFS ≥6 months or Ki-67 ≤20% derived greater benefit: mPFS 7.5 vs. 6.0 months [hazard ratio (HR) 0.38, 95% CI: 0.16-0.91, P=0.03] and 8.5 vs. 6.7 months (HR 0.29, 95% CI: 0.10-0.82, P=0.02), respectively. All other subgroups demonstrated consistent PFS benefit. Any-grade AEs occurred in 56.9% of patients. Myelosuppression (mainly neutropenia and anemia; thrombocytopenia was uncommon) and gastrointestinal toxicities (nausea, vomiting, abdominal pain, diarrhea-mostly grade 1-2) were most frequent. Treatment interruption, modification, or discontinuation due to treatment-related AEs was uncommon (12.1%). Metronomic vinorelbine plus anlotinib shows favorable efficacy in HER2- advanced breast cancer without increasing the risk of AEs.

PMID 42170575
Read full article →
PubMedJournal of endocrinological investigation2026-05-22

Icariin prevents ovariectomy-induced osteoporosis by modulating marrow fatty acid metabolism.

Luo Peng P, Guo Mengyao M, Jiang Lei L, Miao Zeyang Z et al.

To investigate icariin's regulation of marrow fatty acid metabolism and stearoyl-CoA desaturase (SCD) indices in preventing ovariectomy-induced osteoporosis. Thirty-six female Sprague-Dawley rats underwent sham surgery or ovariectomy and were treated with either icariin (125 mg/kg/day) or vehicle via oral gavage for 12 weeks, 6 days per week. Bone marrow was collected from tibias for fatty acid profiling via gas chromatography-mass spectrometry. Serum levels of bone-specific alkaline phosphatase (BALP) and tartrate-resistant acid phosphatase 5b (TRACP-5b) were measured using Enzyme-Linked Immunosorbent Assay. Tibial trabecular microstructure was assessed by micro-CT. Ovariectomy significantly altered marrow fatty acid composition, marked by increased palmitic acid (C16:00) and palmitoleic acid (C16:1 n-7), decreased stearic acid (C18:00) and arachidonic acid (C20:4 n-6), and elevated SCD indices. These changes were associated with deteriorated bone microarchitecture and impaired bone turnover. Icariin treatment effectively normalized marrow fatty acid levels, suppressed SCD indices, and consequently attenuated bone loss by improving bone volume fraction, trabecular number, and thickness, while reducing trabecular separation. Additionally, icariin restored the balance of bone turnover markers, increasing BALP and decreasing TRACP-5b. Significant correlations were identified between specific fatty acids and both bone structural parameters and remodeling markers. Icariin attenuates osteoporotic bone loss by preventing ovariectomy-induced disturbances in marrow fatty acid metabolism, particularly through the suppression of SCD indices and normalization of C16:00, C16:1 n-7, and C18:00 levels. This study highlights the critical role of lipid homeostasis in bone integrity and identifies icariin as a promising lipid-modulating candidate for postmenopausal osteoporosis.

PMID 42171674
Read full article →
PubMedZhonghua yi xue za zhi2026-05-21

[Efficacy and safety of eliglustat tartrate in adults with Gaucher disease type 1].

Hu L Y LY, Ren Y S YS, Zhang L L, Yang R R et al.

To evaluate the efficacy and safety of eliglustat tartrate in adult patients with Gaucher disease type 1 (GD1). Adult patients with GD1 confirmed at the First Medical Center of Chinese People's Liberation Army General Hospital were prospectively enrolled from October 2023 to June 2024. They received eliglustat tartrate capsules treatment (oral, 84 mg, twice daily) for 52 weeks. The changes in glucosylsphingosine (Lyso-GL1), hemoglobin and platelet count, liver and spleen volumes, multiples of normal (MN) of liver and spleen volumes were observed before and after treatment, and adverse reactions during treatment were recorded. A total of 5 adult patients with GD1 type were included, and all were identified as extensive metabolizers (EMs) via CYP2D6 genotyping. Following 52 weeks of treatment, Lyso-GL1 levels decreased apparently from baseline. Hemoglobin levels and platelet count also increased. Both liver and spleen volumes decreased, with corresponding reductions in MN. One patient reported mild nausea and anorexia, which resolved spontaneously within 2 d without other adverse events. Eliglustat tartrate demonstrates favorable efficacy and safety in these 5 adult GD1patients with EMs.

PMID 42161615
Read full article →

+9996 more articles available with a free account

Sign up free to view all articles →

Ask about zolpidem tartrate