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tolterodine (Detrol LA / Detrusitol Neo / Detrusitol Retard)

✓ Approved

Pfizer, Inc. · CHRM1 · Small Molecule

What is tolterodine?

tolterodine is a small molecule developed by Pfizer, Inc.. It is approved for therapeutic indications via oral (po).

Drug Profile

Brand NamesDetrol LA, Detrusitol Neo, Detrusitol Retard
CompanyPfizer, Inc.
Drug ClassSmall Molecule
Molecular TargetCHRM1, CHRM2, CHRM3, CHRM4
RouteOral (PO)
StatusApproved
Sources: ClinicalTrials.gov, Pfizer, Inc.

Mechanism of Action

Molecular Targets

tolterodine acts on 4 molecular targets:

CHRM1cholinergic receptor muscarinic 1 (M1, HM1)
CHRM2cholinergic receptor muscarinic 2 (HM2)
CHRM3cholinergic receptor muscarinic 3 (HM3, PBS)
CHRM4cholinergic receptor muscarinic 4 (HM4, M4R)
Want deeper analysis?Noah AI can explain complex mechanisms and compare to similar drugs.

Therapeutic Indications

tolterodine is developed for 2 unique indications across 1 therapeutic area.

Therapeutic AreaConditionPhase
Renal and urinary disordersHypertonic bladder✓ Approved
Renal and urinary disordersUrinary incontinence✓ Approved

Related Research Articles

PubMedDrug development and industrial pharmacy2026-08-30

Development of Extended-Release Oral Dosage Forms of Salbutamol Sulfate Using the Hot-Melt Extrusion Manufacturing Technique.

Ramadan Banan B, Al-Zoubi Nizar N, Migdadi Eman E, AlSuwais Alia Kh AK et al.

To fabricate and characterize extrudable polymeric matrices using a combination of ethyl cellulose (EC) and two different grades of hydroxypropyl cellulose (HPC) that can provide sustained drug release of the model drug salbutamol sulfate. Implementation of the Hot-Melt Extrusion (HME) technique in the fabrication of polymeric combinations that will provide ready-to-use matrices for sustained release dosage forms. Two formulation groups were developed; each with six formulations. The first group contained EC: HPC 370,000 ratios ranging from 55.52:13.8% to 6.9:62.46%, respectively. The second group contained EC: HPC 80,000 ranging from 59.4:10% to 9.4:60%, respectively. The release profiles were determined via in vitro studies to assess the ability of matrices to prolong salbutamol release. Solid-state characterization was also performed on the raw material and representative extrudates formulations using differential scanning calorimetry (DSC) and X-ray powder diffraction (XRPD) and polarized light microscopy (PLM). The first group formulations exhibited prolonged drug release profiles that accelerated progressively as the level of HPC 370,000 increased. In contrast, the second group formulations exhibited a noticeably faster release, demonstrating that HPC 80,000 can effectively accelerate drug release through enhanced matrix erosion and water penetration. DSC and XRPD revealed that the model drug remained in its stable crystalline state even after thermal processing via HME. PLM further confirmed drug crystallinity within the extrudates. EC-HPC matrices successfully demonstrated the feasibility of using HME to prepare sustained-release matrices for salbutamol sulfate with the ability to tune drug release by varying polymer grade and ratio.

PMID 42669207
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PubMedInternational journal of pharmaceutics2026-08-30

Intranasal delivery of Semaglutide using a thermoresponsive PNPHO nanocarrier: formulation development, characterization and biological evaluation.

Sayka Khan Tanisha Tabassum TT, Jerry Wong Chun Yuen CY, Sheikh Zara Z, Fathi Ali A et al.

Semaglutide (SMG) is a glucagon-like peptide-1 receptor agonist with a promising efficacy and safety profile that is widely used for reducing obesity by targeting the appetite control centres in the brain and for type 2 diabetes management by enhancing insulin release and suppressing glucagon secretion. SMG is currently administered subcutaneously that is invasive with reduced patient compliance or orally leading to decreased efficacy owing to first-pass effects. In this study, a nanoparticle (NP) formulation of SMG was developed using a thermoresponsive and biocompatible synthetic polymer, PNPHO (poly(N-isopropylacrylamide-co-(N-acryloxysuccinimide)-co-(polylactide/-hydroxy methacrylate)-co-(oligo (ethylene glycol)), to investigate its potential to enhance nasal mucosal absorption and prolong residence time via the needle-free intranasal (IN) route. The NP formulation was characterized in vitro for physicochemical parameters, stability, mucoadhesion, regional nasal deposition, drug release profile, and cellular permeation, and in vivo for glucose sensitivity and biodistribution. Monodispersed NPs displayed an average size of 26.14 ± 0.19 nm, a negative surface charge with high SMG encapsulation (89%), improved stability against enzymatic degradation and increased permeation across nasal epithelial cells in vitro compared to SMG alone (p < 0.0001). In contrast, it reduced transport across hCMEC/D3 BBB cells. Nasal cast studies revealed greater NP deposition in the turbinates compared to the free drug. In vivo, the NP formulation demonstrated prolonged nasal retention of the formulation within the sinus region along with an improved glucose tolerance with a 24 h dosing regimen, showing an extended period of pharmacological activity that can be utilized for reducing dosing frequency. No detectable brain fluorescence was observed in vivo. Overall, these findings corroborate the potential of IN delivery of thermoresponsive SMG-PNPHO NP formulation with increased efficacy compared to current SMG delivery modes.

PMID 42669320
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PubMedbioRxiv : the preprint server for biology2026-08-30

Evolutionary rise of a synaptic mechanism for creating and diversifying key reinforcement signals.

Rodriguez-Sosa Natalia N, Rios Lupita L, Lin You-Hsin YH, Rybalchenko Volodymyr V et al.

Most neurons release either excitatory or inhibitory neurotransmitters. However, multiple inputs to the lateral habenula (LHb) co-transmit glutamate and GABA, transmitters with opposing effects on LHb output. Although the LHb has an established role in reinforcement learning, the adaptive significance of glutamate/GABA co-release remains unclear. Using experimentally informed simulations, we show that GABA co-release is sufficient to produce temporal difference (TD)-like transformations of input activity, computations commonly used for reinforcement learning and behavioral optimization. Heterogeneous GABA-to-glutamate ratios, like those found among LHb neurons ex vivo, produce diverse TD-like computations linked to higher-order decision-making. Single-cell RNA-sequencing analysis and machine-learning image analysis further indicate that glutamate/GABA co-release expanded across vertebrate evolution, from fish to mice, rats, and monkeys. Evolutionary expansion of glutamate/GABA co-release may have supported increasingly sophisticated learning and decision-making that contribute to intelligent behavior.

PMID 42668468
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PubMedNeuroscience2026-08-30

Incubation of cocaine craving is associated with reduced context-induced Fos expression in parvalbumin interneurons in the nucleus accumbens core of male rats.

Anesio Augusto A, Lopes Costa Giovanna Victoria GV, Palombo Paola P, Zaniboni Caroline Riberti CR et al.

Substance use disorder develops in a subset of individuals after repeated drug exposure and is characterized by escalating intake and loss of control over use. Rodent self-administration protocols with varying drug access durations are used to study controlled and compulsive drug use and its neurobiology. Drug-associated stimuli are major triggers for relapse. In humans, the craving response elicited by these stimuli progressively increases during abstinence, contributing to high relapse rates. In animals, an analogous process is observed, termed incubation of cocaine craving, which is characterized by a progressive increase in context-induced drug-seeking behavior over the course of abstinence. Associative learning between environmental stimuli and drug use is encoded by neuronal ensembles reactivated by drug-related stimuli, driving drug seeking. In the NAcc, these ensembles regulate cue-driven behaviors, while PV interneurons provide inhibitory control over network activity. We examined overall NAcc and PV-specific recruitment by measuring Fos expression in response to the cocaine-associated context after restricted or extended access self-administration and assessed whether this recruitment is modulated by forced abstinence. The magnitude of context-induced Fos expression in the NAcc core and shell before abstinence was influenced by the amount of cocaine intake during training, with greater expression in extended access rats. NAcc core and shell Fos expression increased after 30 days of abstinence in both groups but was consistently higher in extended access rats. PV Fos expression decreased in extended access rats following forced abstinence. These findings suggest that the Incubated cocaine craving alters NAcc and PV interneuron recruitment.

PMID 42669377
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PubMedFood chemistry: X2026-08-30

Effect of solid-state fermentation on the release and antioxidant activity of soluble polyphenols from wheat bran.

Tian Xiaomin X, Guo Yuqiu Y, Sun Linlin L, Chen Lirong L et al.

Using wheat bran as substrate, four solid-state fermentation methods were compared for soluble polyphenol release. The effect of Bio-enzymatic synergy (BES) is the most significant, producing 4.85 mg GAE/g of total phenolic substances, which is 45.77% higher than the control group (CK). LC-MS analysis revealed that ferulamide and 2,4,6-trihydroxybenzoic acid predominated in positive ion mode, while salicylic acid dominated in negative mode. Notably, salicylic acid was found almost exclusively in ester-bound and glycoside-bound fractions (>88%), indicating its release requires cleavage of covalent linkages to cell wall components. The release of salicylic acid results from the synergistic action of Bio-enzymatic synergy and alkaline hydrolysis. Both in vitro and in vivo assays confirmed that BES-released polyphenols enhanced antioxidant activity, reducing ROS and MDA levels while increasing GSH-Px activity and extending C. elegans lifespan. These findings provide a mechanistic basis for developing targeted fermentation-enzymatic processes to produce functional wheat bran extracts.

PMID 42668496
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PubMedJournal of materials chemistry. B2026-08-30

Fabrication of bilayer nerve conduits with sustained drug release using a multi-material, embedded 3D printing strategy.

Cai Betty B, Ghorbani Sadegh S, He Lili L, Kilian David D et al.

Nerve conduits are commonly used in peripheral nerve repair, but clinically available conduits offer limited functional recovery. While three-dimensional (3D) printing has emerged as a promising technique for nerve conduit fabrication, the fabrication of conduits with both geometrical complexity and biochemical guidance remains challenging. Here, we introduce a multi-material, embedded 3D printing approach to fabricate bilayer nerve conduits capable of sustained drug release. In this approach, bilayer conduits are formed by sequentially extruding two crosslinker-containing inks - a biomaterial ink and a sacrificial ink - into a photocrosslinkable gel precursor support bath. As a demonstration, we fabricated conduits with a gelatin methacryloyl (GelMA)/poly(ethylene glycol) diacrylate (PEGDA)-based outer layer and fibrin-based inner layer. A decoupling of drug delivery and mechanical support is uniquely enabled by the bilayer design, where the outer layer provides mechanical strength and stability, while the inner layer enables the sustained release of nerve growth factor (NGF). The mechanical properties of bilayer conduits with varying diameters were characterized by compressive testing, and drug delivery from bilayer conduits with NGF loaded in the inner layer was quantified using in vitro NGF release and bioactivity assays. Finally, we demonstrated the fabrication of bilayer conduits with branched and multi-lumen geometries, which are challenging to fabricate with existing strategies. Altogether, these results highlight the promise of 3D printed nerve conduits leveraging tunable biomaterials to both physically guide and biochemically promote nerve regeneration.

PMID 42669288
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