Drug Database
TH

theophylline (Contiphyllin / Diffumal 24)

✓ Approved

Lindopharm · ADORA1 · Small Molecule

What is theophylline?

theophylline is a small molecule developed by Lindopharm. It is approved for therapeutic indications via oral (po).

Drug Profile

Brand NamesContiphyllin, Diffumal 24
CompanyLindopharm
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 1 unique indication across 1 therapeutic area.

Therapeutic AreaConditionPhase
Respiratory, thoracic and mediastinal disordersAsthma✓ Approved

Related Research Articles

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.

PubMedDrug metabolism and disposition: the biological fate of chemicals2026-08-06

3D hepatic spheroid arrays for clearance assessment of small and bRo5 molecules.

Mehta Viraj V, Yellanki Rupa R, Molgara Parusharamulu P, Uthukam Venkatesham V et al.

Accurately predicting hepatic clearance remains a critical hurdle in preclinical pharmacokinetics, especially for metabolically stable compounds and emerging modalities such as proteolysis targeting chimeras (PROTACs) that fall in beyond-rule-of-five chemical space. In this study, we developed and evaluated a 3-dimensional hepatic spheroid-array system that improves clearance prediction for both small molecules and PROTACs. Using a panel of 15 small molecules and 9 PROTACs, we compared in vitro clearance predictions from the spheroid-array model with conventional suspension hepatocytes. The spheroid-array predicted human hepatic clearance within a 2-fold range for 9 of 15 and within a 3-fold range for 12 of 15 small molecules. The average absolute fold error was lower for the spheroid system than the suspension system (1.74 vs 3.52). Notably, unlike the suspension system, the spheroid-array quantified clearance for several low-clearance compounds such as warfarin and theophylline. Regression correction improved prediction accuracy for both, with a significant improvement for the suspension model. For several PROTACs, metabolic turnover could not be measured in the suspension system, highlighting its limited suitability for highly stable compounds. In contrast, the spheroid system demonstrated significant metabolic activity, enabling characterization of hepatic clearance for these otherwise stable PROTACs. Together, these findings establish the spheroid-array system as a sensitive and physiologically relevant tool for preclinical clearance assessment across traditional and emerging therapeutic modalities. SIGNIFICANCE STATEMENT: We developed a 3-dimensional hepatic spheroid-array that shows excellent viability and functional activity for 3 weeks. The system showed better hepatic clearance predictivity with a lower average absolute fold error than the suspension system. Our work also first time validates the spheroid-array system for beyond-rule-of-five molecules showing the possibility for evaluating clearance of proteolysis targeting chimeras. This work establishes spheroid as a reliable tool for preclinical hepatic clearance assessment.

PubMedRSC advances2026-08-02

Selective cytotoxicity of [Cu(theophylline)(H2O)2Cl2] complex toward cancer cells: insights from structural, spectroscopic, and molecular docking analyses.

Domingos Francisco N B FNB, de Oliveira Neto João G JG, Rodrigues Jéssica A O JAO, Viana Jailton R JR et al.

The diaquadichlorotheophylline-copper(ii) coordination complex, [Cu(theophylline)(H2O)2Cl2], was synthesized via slow solvent evaporation and comprehensively characterized through experimental and computational approaches. X-ray powder diffraction and Rietveld refinement confirmed a triclinic crystal system (space group P1̄(C 1 i )) with pentacoordinate copper(ii) in a square-pyramidal geometry. Thermal analyses revealed thermal stability up to 358 K, with dehydration requiring 89.5 kJ mol-1 per H2O molecule. Vibrational spectroscopy (Fourier transform infrared and Raman) combined with density functional theory calculations (PBE1PBE/6-311++G(d,p)) provided suitable mode assignments and demonstrated excellent agreement between experimental and calculated spectra, including solvent effects using the IEFPCM model. Frontier molecular orbital analysis yielded the highest occupied molecular orbital-lowest unoccupied molecular orbital gaps of approximately 3.8 eV and electrophilicity indices of approximately 6.8 eV, indicating good chemical stability and biological potential. Ultraviolet-visible-near infrared spectroscopy revealed characteristic d-d transitions for pentacoordinate copper(ii) and π → π*/n → π* transitions from the theophylline ligand. Molecular docking predicted a strong in silico binding affinity to deoxyribonucleic acid (K i = 5.85 µM, binding free energy = -7.14 kcal mol-1), consistent with an intercalative mode and moderate affinity to bovine serum albumin (K i = 40.78 µM, binding free energy = -5.99 kcal mol-1). Cytotoxicity assays against PC-3 (prostate), MDA-MB-231 (breast), and HCT-116 (colorectal) cancer cell lines revealed dose-dependent activity with half-maximal inhibitory concentration values ranging from 2.91 to 3.77 µM and selectivity indices greater than 1 compared to the non-tumorigenic GM07429A cell line, with preferential activity against breast cancer. These results indicate that diaquadichlorotheophylline-copper(ii) is a promising anticancer candidate with favorable selectivity for malignant cells over healthy tissue, warranting further preclinical evaluation.

PubMedScientific reports2026-08-01

Impact of blood collection tubes on thrombin generation assay results: a comparison of citrate and CTAD.

Ulbing Stefan S, Schäfer Fabian F, Koch Stefan S, Dibiasi Christoph C et al.

Accurate assessment of haemostasis is essential in both research and clinical practice. Thrombin generation assays (TGA) provide a comprehensive evaluation of coagulation; however, results can be influenced by preanalytical conditions, including the choice of blood collection tubes. Citrate-theophylline-adenosine-dipyridamole (CTAD) tubes are recommended by the manufacturer of the Ceveron® alpha TGA system due to their ability to inhibit platelet activation. Nevertheless, CTAD tubes are costly, less widely available, and not manufactured in small volumes suitable for specific patient populations, such as paediatric cohorts. To evaluate whether standard citrate tubes can serve as a viable alternative, we prospectively compared TGA parameters from blood collected in 3.2% sodium citrate tubes versus CTAD tubes in 12 healthy volunteers. Assays were performed using low and high phospholipid micelle concentrations (RC low/RC high). Significant differences between citrate and CTAD were observed for all parameters with the RC low reagent. In contrast, only lag time showed significant differences with the RC high reagent. In conclusion, while citrate tubes may be used for TGA, the type of blood collection tube can influence measurements under specific assay conditions and should be considered a relevant factor when comparing and interpreting TGA results.

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