Drug Database
TH

theophylline (Unifyl / Uniphyllin / theophylline, Napp)

✓ Approved

Purdue Pharma L.P. · ADORA1 · Small Molecule

What is theophylline?

theophylline is a small molecule developed by Purdue Pharma L.P.. It is approved for therapeutic indications via oral (po).

Drug Profile

Brand NamesUnifyl, Uniphyllin, theophylline, Napp
CompanyPurdue Pharma L.P.
Drug ClassSmall Molecule
Molecular TargetADORA1, ADORA2A
RouteOral (PO)
StatusApproved

Mechanism of Action

Molecular Targets

theophylline acts on 2 molecular targets:

ADORA1adenosine A1 receptor (RDC7)
ADORA2Aadenosine A2a receptor (A2aR, RDC8)
Want deeper analysis?Noah AI can explain complex mechanisms and compare to similar drugs.

Therapeutic Indications

theophylline is developed for 3 unique indications across 1 therapeutic area.

Therapeutic AreaConditionPhase
Respiratory, thoracic and mediastinal disordersAsthma✓ Approved
Respiratory, thoracic and mediastinal disordersBronchitis chronic✓ Approved
Respiratory, thoracic and mediastinal disordersChronic obstructive pulmonary disease✓ Approved

Related Research Articles

PubMedInternational journal of molecular sciences2026-08-27

Computational Analysis of Sequence Editability in the Theophylline RNA Aptamer as a Functional RNA Module.

Aman Aamir A, Sidl Leonhard L, Darai Nitchakan N, Wolschann Peter P et al.

RNA aptamers are often used as ligand-recognition modules in engineered RNA systems, but integration into larger RNA constructs can influence stability and ligand binding. As a result, aptamer sequences may need to be adapted to new environments while preserving essential properties. Here, we examine this sequence editability problem for the theophylline RNA aptamer. Starting from the experimentally determined structure, we introduced targeted mutations in peripheral structural elements while leaving the recognition site unchanged. The native aptamer, mutated variants, a Mg2+-depleted system, and a caffeine-bound control were analyzed using three independent 1 μs molecular dynamics simulations. Binding energetics were estimated with multiple end-point as well as alchemical free energy approaches. Results were interpreted together with base pair stability, the conformational landscape of the binding pocket, and per-nucleotide energy contributions. This allows us to predict whether an edit is tolerated or disruptive. Some mutations retained structural and energetic profiles comparable to the native aptamer, whereas others reduced ligand affinity by propagating structural distortions into the binding pocket. These results show that sequence changes outside the binding site can modulate ligand binding indirectly, and that the ligand interaction network is useful for evaluating edited aptamers. The introduced workflow provides a novel combination of established computational strategies for efficient in silico screening of aptamer variants before experimental testing and can be integrated into the design of larger RNA structures. This works particularly well when an experimental structure is available and the tested mutations are small enough not to disrupt the folding pathway.

PubMedPharmaceutics2026-08-27

Comprehensive Evaluation of Storage Stability and Cytotoxicity of Co-Spray-Dried Theophylline Dry Powders for Inhalation: Follow-Up Study.

Soliman Lomass L, Paróczai Dóra D, Burián Katalin K, Ambrus Rita R

Background/Objectives: The stability and biological safety of newly developed formulations must be established to support their therapeutic efficacy and clinical translation in pulmonary drug delivery. Therefore, this follow-up study comprehensively evaluated the short- and long-term stability and the in vitro cytotoxicity of optimized, co-spray-dried theophylline (THN) dry powders for inhalation against A549 lung epithelial cells. Methods: Two established formulations were selected: THN-RAF (raffinose-leucine-glycine based) and THN-TRE (trehalose-leucine based). Stability was assessed under accelerated conditions (40 °C/75% RH, 3 months) and long-term desiccator storage (25 °C, 1 year) using laser diffraction, SEM, XRPD, FTIR, DSC, TGA, and Andersen Cascade Impaction. As THN-TRE had been previously confirmed to be cytocompatible, only THN-RAF and its components were evaluated against A549 human alveolar epithelial cells using the MTT assay. Results: Under accelerated conditions, both formulations exhibited pronounced recrystallization (Xc up to 89.9%), agglomeration (D [0.9] up to 217.08 µm for THN-TRE), and deterioration in aerodynamic performance (FPF as low as 11.55%, MMAD up to 6.68 µm). By contrast, long-term desiccator storage induced substantial recrystallization (Xc up to 80.7%) while preserving thermal, chemical, and aerodynamic performance (FPF ≈ 40%; MMAD 4.99-5.21 µm). THN-RAF was more resistant to stress-induced agglomeration than THN-TRE. Cytotoxicity assessment confirmed cytocompatibility of THN-RAF, with cell viability exceeding 70.99% at all tested concentrations (up to 500 µg/mL). Conclusions: These findings reveal a marked discrepancy between the outcomes of ICH accelerated testing and long-term desiccator storage. They underscore the importance of considering moisture-protective packaging configurations when designing stability protocols for amorphous inhalable formulations.

PubMedRespirology case reports2026-08-27

Shrinking Lung Syndrome in Adolescent Systemic Lupus Erythematosus: Diagnostic Utility of Diaphragmatic Ultrasound.

Farid Ayesha A, Basit Abdul A, Rana Ali Raza AR, Ahmed Sharaz S et al.

Shrinking lung syndrome (SLS) is a rare pulmonary complication of systemic lupus erythematosus (SLE), characterized by dyspnoea, reduced lung volumes, and elevated diaphragms without significant parenchymal lung disease. We report a 17-year-old female with SLE presenting with progressive dyspnoea, dry cough, and pleuritic chest pain. Pulmonary function tests showed a restrictive defect (forced vital capacity 39% predicted) with preserved diffusing capacity. High-resolution computed tomography demonstrated reduced lung volumes with bilateral diaphragmatic elevation and basal atelectasis, without interstitial lung disease. Diaphragmatic ultrasound revealed reduced excursion and decreased thickening fraction, indicating diaphragmatic dysfunction. Alternative cardiopulmonary and neuromuscular causes were excluded, establishing the diagnosis of SLS. The patient was treated with corticosteroids and theophylline, resulting in symptomatic improvement. This case highlights the importance of recognizing SLS and demonstrates the diagnostic value of diaphragmatic ultrasound as a non-invasive tool facilitating early diagnosis and management.

PubMedMedical research archives2026-08-25

Protective versus Risk Factors for 18-month Outcomes in a multi-decade sample of preterm infants age 23-30 weeks.

Rosenkrantz Ted S TS, McLeod Ruth M RM, Fitch R Holly RH

This paper summarizes risk and protective factors modulating cognitive, language and motor outcomes in a cohort of preterm infants from Connecticut Children's Medical Center and University of Connecticut Health Center. Infants were born at 23-30 weeks gestational age and admitted to the neonatal unit (1991 - 2017). Extracted and de-identified patient data included sex, gestational age (GA), birthweight, maternal health conditions (pre-eclampsia, diabetes, etc.), presence of necrotizing enterocolitis, intra-ventricular hemorrhage and grade, maternal magnesium sulfate (MGS) treatment, and administration of the methylxanthine (MX) adenosine antagonists (caffeine or theophylline) and timing (< 48 hrs from birth (early) or > 48 hrs (late)). Outcome measures were obtained at 18-month follow-up evaluations (Bayley Scale and/or Cognitive Adaptive Test/Clinical Linguistic and Auditory Milestone Scale). Scores on different components of the tests were z-scored and averaged into 3 categories for each infant as Language, Cognitive, and Motor indices. Significant risk factors for poor outcomes were found to include: (1) being male, (2) extremely low birthweight (a better predictor of poor outcome than low GA), (3) positive inflammatory perinatal profile; and (4) MGS exposure in males, particularly when followed by early MX treatment. Factors leading to significantly better outcomes included: (1) MX exposure within 48 hours of birth, particularly in infants with inflammation (but excluding males with prior MGS exposure); and (2) perinatal MGS exposure, particularly in lower birthweight females (but excluding early MX-treated males). This novel evidence of sub-group specific therapeutic benefits and harms emphasizes a serious need for additional research on individualized therapeutic interventions for at-risk preterm infants and reveals a novel deleterious interaction between magnesium sulfate exposure and subsequent treatment with methyxanthines (e.g., caffeine) within 48 hours of birth for preterm boys.

PubMedThe Cochrane database of systematic reviews2026-08-20

Methylxanthines for the prevention or treatment of intermittent hypoxemia or respiratory insufficiency in late preterm infants.

Bodrero Enrico E, Isaza-López María Carolina MC, Pahl Adrienne A, Fiander Michelle M et al.

Late preterm infants (34 0/7 to 36 6/7 weeks' gestation, i.e. 34 weeks and 0 days to 36 weeks and 6 days) are at increased risk of intermittent hypoxemia and respiratory insufficiency due to physiological immaturity, compared to full-term infants. Methylxanthines, most frequently caffeine, are used to improve respiratory function and long-term outcomes in very preterm infants. However, the use of methylxanthines in late preterm infants for preventing or treating intermittent hypoxemia and respiratory insufficiency needs to be assessed, also to avoid the risk of over-treatment. To assess the benefits and harms of methylxanthines in preventing or treating intermittent hypoxemia or respiratory insufficiency in late preterm infants. Searches were conducted up to December 2025 in MEDLINE, CENTRAL, Embase, Epistemonikos, and two clinical trial registries. We also screened the reference lists of relevant reviews and included studies. We included randomized controlled trials enrolling late preterm infants, comparing any methylxanthine (aminophylline, theophylline, or caffeine) with placebo or no methylxanthine. Studies with a cross-over design were excluded. Critical outcomes were the number of intermittent hypoxemia episodes and apnea after 24 hours and over one week from starting treatment, and major neurodevelopmental disability. Important outcomes included respiratory support, duration of hospital stay, all-cause mortality prior to discharge, and adverse effects leading to treatment discontinuation. We assessed risk of bias using the Cochrane RoB 2 tool. We used a fixed-effect model to calculate risk ratios (RRs) with 95% confidence intervals (CIs) for the outcomes: respiratory support, all-cause mortality before discharge, and adverse effects leading to treatment discontinuation. For intermittent hypoxemia and duration of hospital stay, we calculated ratios of geometric means. We assessed the certainty of the evidence using GRADE methods. Study authors were contacted for additional data when required. We included one randomized controlled trial involving 132 late preterm infants in New Zealand. Infants were assigned to receive either caffeine or placebo for the prevention of intermittent hypoxemia. Reported outcomes included episodes of intermittent hypoxemia, respiratory support, duration of hospital stay, all-cause mortality, and adverse effects leading to treatment discontinuation. No eligible studies assessed methylxanthines for the treatment of intermittent hypoxemia, apnea, or respiratory insufficiency. We identified five ongoing trials: the largest is expected to enroll 478 late preterm infants and to be completed in 2026. The included study did not report the critical outcome of the number of episodes of intermittent hypoxemia after 24 hours from starting treatment (i.e. from day two through the end of the first week). Methylxanthines may reduce the number of episodes of intermittent hypoxemia over one week from starting treatment compared to placebo or no treatment (ln [ratio of geometric means] -0.58, 95% CI -1.14 to -0.02; I² not applicable; 1 study, 132 participants; low-certainty evidence). The evidence is very uncertain about the effect of methylxanthines on respiratory support after 24 hours from starting treatment (RD 0.00, 95% CI -0.05 to 0.05; I² not applicable; 1 study, 132 participants; very low-certainty evidence); on duration of hospital stay (ln [ratio of geometric means] 0.23, 95% CI -0.01 to 0.47; I² not applicable; 1 study, 132 participants; very low-certainty evidence); and on any adverse effects leading to treatment discontinuation at the end of study compared to placebo or no treatment (RR 2.57, 95% CI 0.65 to 10.22; I² not applicable; 1 study, 132 participants; very low-certainty evidence). Methylxanthines may result in little to no difference in all-cause mortality prior to hospital discharge compared to placebo or no treatment (RD 0.00, 95% CI -0.05 to 0.05; I² not applicable; 1 study, 132 participants; low-certainty evidence). No studies reported on apnea or major neurodevelopmental disability. The certainty of the evidence is limited by the inclusion of only one study, with all outcomes downgraded for serious or very serious imprecision. For most outcomes, we also downgraded the certainty of the evidence due to some concerns about the risk of bias. These findings should be considered preliminary and are likely to change with future research. Overall, methylxanthine therapy in late preterm infants may reduce the number of intermittent hypoxemia episodes over one week from starting treatment, but likely results in little to no difference in all-cause mortality prior to hospital discharge. The effects of methylxanthines on other important outcomes, such as respiratory support, duration of hospital stay and adverse effects, remain highly uncertain due to limited and low-certainty evidence. A few outcomes were not reported, and no studies addressed the treatment of established intermittent hypoxemia or respiratory insufficiency. Current evidence is limited, and further high-quality trials are needed to clarify the efficacy and safety of methylxanthines in late preterm infants. The identified ongoing trials are planning to recruit over 900 infants, with the largest (n = 478) expected to be completed in 2026. This Cochrane review was supported by Cochrane Sweden, Region Skåne and Skåne University Hospital, Lund University, and Vermont Oxford Network. No dedicated funding was received. Protocol (2024) DOI: 10.1002/14651858.CD016113.

PubMedMethods in molecular biology (Clifton, N.J.)2026-08-19

A Conditional Plasmid System for Markerless Gene Deletion in Genetically Recalcitrant Fusobacterium nucleatum subsp. animalis.

G C Bibek B, Wu Chenggang C

Fusobacterium nucleatum subsp. animalis (FNA) plays a prominent role in oral microbial ecology and is increasingly implicated in systemic diseases such as colorectal cancer. However, its genetic intractability has significantly hindered functional studies to understand its pathogenic mechanisms. To address this challenge, we developed a conditional plasmid system that enables efficient, markerless gene deletion in FNA strains. This system features inducible control of plasmid replication via a theophylline-responsive riboswitch regulating repA, and counterselection via the MazF toxin under the control of an anhydrotetracycline-inducible promoter. In this chapter, we provide a detailed, step-by-step protocol for implementing this system using FNA strain 7_1 as a model. We illustrate the procedure by deleting the luxS gene, which encodes S-ribosylhomocysteine lyase-an enzyme involved in AI-2 quorum sensing and biofilm regulation. Our protocol provides a powerful and adaptable tool for advancing genetic studies in this genetically recalcitrant subspecies.

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