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Theophylline | CAS No: 58-55-9 | GMP-certified suppliers
A medication that relieves symptoms and reversible airflow obstruction in chronic asthma, chronic bronchitis, and emphysema, supporting consistent management of obstructive lung diseases.
Therapeutic categories
Agents that reduce seizure thresholdAlkaloidsAnti-Asthmatic AgentsAutonomic AgentsBronchodilator AgentsCardiovascular Agents
Generic name
Theophylline
Molecule type
small molecule
CAS number
58-55-9
DrugBank ID
DB00277
Approval status
Approved drug
ATC code
R03DA54
Primary indications
- For the treatment of the symptoms and reversible airflow obstruction associated with chronic asthma and other chronic lung diseases, such as emphysema and chronic bronchitis
Product Snapshot
- Theophylline is a small‑molecule API supplied primarily in oral immediate‑ and extended‑release forms, with additional injectable and inhalation presentations
- It is used for managing symptoms and reversible airflow obstruction in chronic asthma and other chronic obstructive pulmonary diseases
- It is an approved product in the United States and Canada
Clinical Overview
Theophylline (CAS 58-55-9) is a methylxanthine bronchodilator indicated for symptomatic treatment of reversible airflow obstruction in chronic asthma, chronic bronchitis, and emphysema. It is widely used in the management of obstructive airway diseases where sustained bronchodilation and modulation of airway reactivity are required. Theophylline is available globally in multiple modified‑release formulations, including long‑established brands such as Uniphyl and Theochron.
Pharmacologically, theophylline is a xanthine derivative structurally related to caffeine and theobromine. Its therapeutic effects in the airways involve smooth muscle relaxation and attenuation of airway responsiveness to environmental and inflammatory stimuli. These combined bronchodilator and non‑bronchodilator actions contribute to improvement in airflow and symptom control in patients with reversible obstruction.
The mechanism of action is multimodal. Theophylline competitively inhibits phosphodiesterase isoenzymes, particularly PDE III and PDE IV, leading to increased intracellular cyclic AMP and relaxation of bronchial and vascular smooth muscle. It also antagonizes adenosine A2B receptors, counteracting adenosine‑mediated bronchoconstriction. In inflammatory contexts, theophylline can activate histone deacetylase, supporting repression of pro‑inflammatory gene transcription.
Theophylline exhibits variable oral absorption depending on formulation. It distributes widely and crosses the placenta and into breast milk. Metabolism occurs primarily via hepatic cytochrome P450 pathways, especially CYP1A2, with contributions from CYP2E1, CYP2D6, CYP2C8, and CYP3A4. Clearance is influenced by age, smoking status, hepatic function, and interacting drugs. The compound has a narrow therapeutic index, and plasma concentration monitoring is commonly required to minimize toxicity.
Safety considerations include dose‑related gastrointestinal effects, CNS stimulation, arrhythmias, and seizure risk. Elevated levels increase the likelihood of serious adverse events due to the narrow therapeutic window and extensive drug–drug interaction profile.
For API procurement, sourcing teams should verify compliance with pharmacopoeial specifications, ensure control of polymorphic form and particle size distribution for formulation performance, and confirm robust impurity profiles and supplier GMP adherence.
Pharmacologically, theophylline is a xanthine derivative structurally related to caffeine and theobromine. Its therapeutic effects in the airways involve smooth muscle relaxation and attenuation of airway responsiveness to environmental and inflammatory stimuli. These combined bronchodilator and non‑bronchodilator actions contribute to improvement in airflow and symptom control in patients with reversible obstruction.
The mechanism of action is multimodal. Theophylline competitively inhibits phosphodiesterase isoenzymes, particularly PDE III and PDE IV, leading to increased intracellular cyclic AMP and relaxation of bronchial and vascular smooth muscle. It also antagonizes adenosine A2B receptors, counteracting adenosine‑mediated bronchoconstriction. In inflammatory contexts, theophylline can activate histone deacetylase, supporting repression of pro‑inflammatory gene transcription.
Theophylline exhibits variable oral absorption depending on formulation. It distributes widely and crosses the placenta and into breast milk. Metabolism occurs primarily via hepatic cytochrome P450 pathways, especially CYP1A2, with contributions from CYP2E1, CYP2D6, CYP2C8, and CYP3A4. Clearance is influenced by age, smoking status, hepatic function, and interacting drugs. The compound has a narrow therapeutic index, and plasma concentration monitoring is commonly required to minimize toxicity.
Safety considerations include dose‑related gastrointestinal effects, CNS stimulation, arrhythmias, and seizure risk. Elevated levels increase the likelihood of serious adverse events due to the narrow therapeutic window and extensive drug–drug interaction profile.
For API procurement, sourcing teams should verify compliance with pharmacopoeial specifications, ensure control of polymorphic form and particle size distribution for formulation performance, and confirm robust impurity profiles and supplier GMP adherence.
Identification & chemistry
| Generic name | Theophylline |
|---|---|
| Molecule type | Small molecule |
| CAS | 58-55-9 |
| UNII | 0I55128JYK |
| DrugBank ID | DB00277 |
Pharmacology
| Summary | Theophylline is a xanthine derivative that exerts bronchodilatory and airway‑modulating effects through inhibition of phosphodiesterase enzymes and antagonism of adenosine receptors. These actions elevate intracellular cyclic AMP and reduce adenosine‑mediated bronchoconstriction, diminishing airway smooth‑muscle contraction and responsiveness to inflammatory stimuli. The compound also influences inflammatory gene expression through histone deacetylase activation. |
|---|---|
| Mechanism of action | Theophylline relaxes the smooth muscle of the bronchial airways and pulmonary blood vessels and reduces airway responsiveness to histamine, methacholine, adenosine, and allergen. Theophylline competitively inhibits type III and type IV phosphodiesterase (PDE), the enzyme responsible for breaking down cyclic AMP in smooth muscle cells, possibly resulting in bronchodilation. Theophylline also binds to the adenosine A2B receptor and blocks adenosine mediated bronchoconstriction. In inflammatory states, theophylline activates histone deacetylase to prevent transcription of inflammatory genes that require the acetylation of histones for transcription to begin. |
| Pharmacodynamics | Theophylline, an xanthine derivative chemically similar to caffeine and theobromine, is used to treat asthma and bronchospasm. Theophylline has two distinct actions in the airways of patients with reversible (asthmatic) obstruction; smooth muscle relaxation (i.e., bronchodilation) and suppression of the response of the airways to stimuli (i.e., non-bronchodilator prophylactic effects). |
Targets
| Target | Organism | Actions |
|---|---|---|
| Adenosine receptor A1 | Humans | antagonist |
| Adenosine receptor A2a | Humans | antagonist |
| Adenosine receptor A2b | Humans | antagonist |
ADME / PK
| Absorption | Theophylline is rapidly and completely absorbed after oral administration in solution or immediate-release solid oral dosage form. |
|---|---|
| Half-life | 8 hours |
| Protein binding | 40%, primarily to albumin. |
| Metabolism | Hepatic. Biotransformation takes place through demethylation to 1-methylxanthine and 3-methylxanthine and hydroxylation to 1,3-dimethyluric acid. 1-methylxanthine is further hydroxylated, by xanthine oxidase, to 1-methyluric acid. About 6% of a theophylline dose is N-methylated to caffeine. Caffeine and 3-methylxanthine are the only theophylline metabolites with pharmacologic activity. |
| Route of elimination | Theophylline does not undergo any appreciable pre-systemic elimination, distributes freely into fat-free tissues and is extensively metabolized in the liver. Renal excretion of unchanged theophylline in neonates amounts to about 50% of the dose, compared to about 10% in children older than three months and in adults. |
| Volume of distribution | * 0.3 to 0.7 L/kg |
| Clearance | * 0.29 mL/kg/min [Premature neonates, postnatal age 3-15 days] * 0.64 mL/kg/min [Premature neonates, postnatal age 25-57 days] * 1.7 mL/kg/min [Children 1-4 years] * 1.6 mL/kg/min [Children 4-12 years] * 0.9 mL/kg/min [Children 13-15 years] * 1.4 mL/kg/min [Children 16-17 years] * 0.65 mL/kg/min [Adults (16-60 years), otherwise healthy non-smoking asthmatics] * 0.41 mL/kg/min [Elderly (>60 years), non-smokers with normal cardiac, liver, and renal function] * 0.33 mL/kg/min [Acute pulmonary edema] * 0.54 mL/kg/min [COPD >60 years, stable, non-smoker >1 year] * 0.48 mL/kg/min [COPD with cor pulmonale] * 1.25 mL/kg/min [Cystic fibrosis (14-28 years)] * 0.31 mL/kg/min [Liver disease cirrhosis] * 0.35 mL/kg/min [acute hepatitis] * 0.65 mL/kg/min [cholestasis] * 0.47 mL/kg/min [Sepsis with multi-organ failure] * 0.38 mL/kg/min [hypothyroid] * 0.8 mL/kg/min [hyperthyroid] |
Formulation & handling
- Suitable for oral and IV formulations; oral products often use extended‑release matrices to manage the narrow therapeutic window and sustain plasma levels.
- High aqueous solubility and low logP support solution and syrup formulations, with attention to pH to maintain solubility and limit degradation.
- Formulation and packaging should consider interactions with alcohol and certain botanicals that can alter clearance, requiring consistent administration relative to food.
Regulatory status
| Lifecycle | The API appears to be in a mature phase in both the US and Canada, where market presence and patent‑expiry timing suggest established competition and limited remaining exclusivity. |
|---|
| Markets | Canada, US |
|---|
Supply Chain
| Supply chain summary | Theophylline is produced by a large number of manufacturers, reflecting the absence of a single dominant originator and the longstanding availability of this agent. Branded and generic products are present primarily in the US and Canada, with historical originator brands now supplemented by extensive repackaging and distribution networks. Patent expiry occurred long ago, so the market already supports broad generic competition. |
|---|
Safety
| Toxicity | Symptoms of overdose include seizures, arrhythmias, and GI effects. |
|---|
High Level Warnings:
- Overexposure may elicit neurotoxic and cardiotoxic responses, including seizure activity and ventricular arrhythmias
- High concentrations can provoke gastrointestinal irritation, requiring controls to limit inhalation or accidental ingestion during handling
- Processing should include monitoring measures for compounds with CNS‑stimulating profiles to prevent acute toxicity events
Theophylline is a type of Bronchodilators
Bronchodilators are a vital category of pharmaceutical active pharmaceutical ingredients (APIs) primarily used in the treatment of respiratory conditions such as asthma and chronic obstructive pulmonary disease (COPD). These medications function by relaxing and widening the airways in the lungs, thus facilitating easier breathing.
Bronchodilators can be classified into two main types: beta-agonists and anticholinergics. Beta-agonists, including drugs like salbutamol and formoterol, work by stimulating beta receptors in the smooth muscles of the airways, leading to their relaxation and dilation. This action allows more air to pass through the bronchial tubes and improves airflow to the lungs.
Anticholinergics, such as ipratropium bromide and tiotropium, function by blocking the action of acetylcholine, a neurotransmitter that contracts the smooth muscles in the airways. By inhibiting the effects of acetylcholine, anticholinergics promote bronchial muscle relaxation, leading to expanded airways and increased airflow.
These bronchodilator APIs are typically formulated into inhalers, nebulizers, or oral medications to deliver the active ingredients directly to the lungs. The precise dosage and administration route may vary based on the severity of the respiratory condition and the patient's individual needs.
Bronchodilators play a crucial role in managing respiratory disorders and improving patients' quality of life. They are commonly prescribed by healthcare professionals and are often used in combination with other medications, such as corticosteroids, to achieve optimal therapeutic outcomes. It is important to note that the use of bronchodilators should be carefully monitored and controlled under the guidance of a healthcare professional to ensure proper efficacy and minimize potential side effects.
Theophylline API manufacturers & distributors
Compare qualified Theophylline API suppliers worldwide. We currently have 5 companies offering Theophylline API, with manufacturing taking place in 4 different countries. Use the table below to review supplier type, countries of origin, certifications, product portfolio and GMP audit availability.
| Supplier | Type | Country | Product origin | Certifications | Portfolio |
|---|---|---|---|---|---|
| Bakul Pharma Private Limi... | Producer | India | India | BSE/TSE, CoA, FDA, GMP, MSDS | 52 products |
| Caesar & Loretz GmbH (CAE... | Distributor | Germany | Unknown | BSE/TSE, CoA, GMP, ISO9001, MSDS | 211 products |
| Shandong Xinhua | Producer | China | China | CEP, CoA, FDA, GMP, JDMF, USDMF, WC | 21 products |
| Shizuoka Coffein Co | Producer | Japan | Japan | CoA, JDMF | 8 products |
| Sinoway industrial Co.,Lt... | Distributor | China | China | CEP, CoA, GMP, ISO9001 | 762 products |
When sending a request, specify which Theophylline API quality you need: for example EP (Ph. Eur.), USP, JP, BP, or another pharmacopoeial standard, as well as the required grade (base, salt, micronised, specific purity, etc.).
Use the list above to find high-quality Theophylline API suppliers. For example, you can select GMP, FDA or ISO certified suppliers. Visit our help page to learn more about sourcing APIs via Pharmaoffer.
Frequently asked questions about Theophylline API
Sourcing
What matters most when sourcing GMP-grade Theophylline?
Key considerations include confirming GMP compliance and alignment with US and Canadian regulatory expectations. Because Theophylline is supplied by many manufacturers, verifying the supplier’s quality management system, audit history, and documentation consistency is important. Traceability through repackagers and distributors should also be assessed to ensure control of the supply chain.
Which documents are typically required when sourcing Theophylline API?
Request the core API documentation set: CoA (5 companies), GMP (4 companies), FDA (2 companies), CEP (2 companies), JDMF (2 companies). Confirm versions and validity dates match the destination market to avoid delays in qualification.
Which manufacturers are known to produce Theophylline API?
Known or reported manufacturers for Theophylline: Caesar & Loretz GmbH (CAELO), Sinoway industrial Co.,Ltd, Bakul Pharma Private Limited. Evaluate their GMP history, scale, and regional coverage before requesting dossiers or allocating demand.
How can I request quotes for Theophylline API from GMP suppliers?
Submit quote requests through the supplier listings with your specs and required documents (specifications, target volume, delivery timeline, and destination). Providing consistent details upfront speeds comparable offers and clarifies technical feasibility.
Is a GMP audit report available for Theophylline manufacturers?
Audit reports may be requested for Theophylline: 2 GMP audit reports available. Confirm the scope and recency of any audit before relying on it for qualification decisions.
How many suppliers offer Theophylline API on Pharmaoffer?
Reported supplier count for Theophylline: 5 verified suppliers. Filter listings by certifications, regions, and delivery options to match your qualification plan.
Which countries are known to manufacture Theophylline API?
Production countries reported for Theophylline: China (2 producers), India (1 producer), Japan (1 producer). Knowing the manufacturing geography helps anticipate logistics lead times and import compliance needs.
Which certifications do suppliers of Theophylline usually hold?
Common certifications for Theophylline suppliers: CoA (5 companies), GMP (4 companies), FDA (2 companies), CEP (2 companies), JDMF (2 companies). Always verify issuing authorities and expiry dates when reviewing audit packages.
Technical
What is Theophylline (CAS 58-55-9) used for?
Theophylline is used for the symptomatic treatment of reversible airflow obstruction in chronic asthma, chronic bronchitis, and emphysema. It provides sustained bronchodilation and reduces airway responsiveness by inhibiting phosphodiesterase enzymes and antagonizing adenosine receptors. These actions support improved airflow and symptom control in obstructive airway diseases.
Which therapeutic class does Theophylline fall into?
Theophylline belongs to the following therapeutic categories: Agents that reduce seizure threshold, Alkaloids, Anti-Asthmatic Agents, Autonomic Agents, Bronchodilator Agents. This positioning helps teams compare alternative APIs, anticipate pharmacology expectations, and align early research priorities.
What conditions is Theophylline mainly prescribed for?
The primary indications for Theophylline: For the treatment of the symptoms and reversible airflow obstruction associated with chronic asthma and other chronic lung diseases, such as emphysema and chronic bronchitis. These use cases frame the target patient populations and help prioritize formulation and safety evaluations.
How does Theophylline work?
Theophylline relaxes the smooth muscle of the bronchial airways and pulmonary blood vessels and reduces airway responsiveness to histamine, methacholine, adenosine, and allergen. Theophylline competitively inhibits type III and type IV phosphodiesterase (PDE), the enzyme responsible for breaking down cyclic AMP in smooth muscle cells, possibly resulting in bronchodilation. Theophylline also binds to the adenosine A2B receptor and blocks adenosine mediated bronchoconstriction. In inflammatory states, Theophylline activates histone deacetylase to prevent transcription of inflammatory genes that require the acetylation of histones for transcription to begin.
What should someone know about the safety or toxicity profile of Theophylline?
Theophylline has a narrow therapeutic index, and elevated plasma levels can lead to dose‑related gastrointestinal irritation, CNS stimulation, seizures, and ventricular arrhythmias. Its neurotoxic and cardiotoxic potential makes concentration monitoring important during use or handling. Processing the API should include controls to limit inhalation or accidental ingestion and monitoring measures appropriate for compounds with CNS‑stimulating properties.
What are important formulation and handling considerations for Theophylline as an API?
Important considerations include maintaining adequate aqueous solubility by controlling formulation pH and selecting excipients that limit degradation. Extended‑release oral matrices are used to sustain plasma concentrations due to the narrow therapeutic window. Consistency with food and avoidance of interacting substances such as alcohol or certain botanicals help maintain predictable clearance. For IV or solution forms, stability and compatibility in aqueous systems should be verified.
Is Theophylline a small molecule?
Theophylline is classified as a small molecule. That classification shapes process design, impurity profiling, and analytical control strategies.
Are there special stability concerns for oral Theophylline?
Oral Theophylline requires control of formulation pH to maintain solubility and limit degradation in solution or syrup forms. Extended‑release matrices must remain intact to provide consistent plasma levels given the narrow therapeutic window. Packaging and use conditions should also minimize exposure to substances such as alcohol or certain botanicals that can alter clearance and affect consistent drug delivery.
Regulatory
Where is Theophylline approved or in use globally?
Theophylline is reported as approved in the following major regions: Canada, US. Understanding geographic coverage informs regulatory filings, supply planning, and risk assessments before escalating procurement.
Pharmaoffer
How does Pharmaoffer’s Smart Sourcing Service help with Theophylline procurement?
Pharmaoffer's Smart Sourcing Service coordinates compliant suppliers, documentation, and competitive quotes for Theophylline. It centralizes outreach, follow-ups, and document validation to shorten procurement timelines.
Is Theophylline included in the PRO Data Insights coverage?
PRO Data Insights coverage for Theophylline: 1370 verified transactions across 377 suppliers and 291 buyers worldwide. Use the dataset to benchmark suppliers and monitor regulatory activity where available.
Where can I access the API market report for Theophylline?
Market report availability for Theophylline: Report Available. The report highlights demand trends, pricing drivers, and supplier landscape insights for procurement planning.
