Theophylline Background Information Theophylline is a colorless crystalline alkaloid that is derived from tea leaves or made synthetically. It is a methylxanthine drug that is similar to caffeine in its structure and pharmacology. Theophylline is used as a bronchial dilator for respiratory diseases such as chronic obstructive pulmonary disease (COPD) or asthma. Theophylline inhibits the TGF-∫ regulated conversion of pulmonary fibroblasts into myofibroblasts via cyclic adenosine monophosphate (cAMP)-PKA pathway, and it suppresses COL1 mRNA which codes for the protein collagen. Theophylline also directly activates histone deacetylase (HDAC), an enzyme that mediates inflammatory responses, and it decreases the levels of interleukin-4 (IL-4) and cyclic guanosine monophosphate (cGMP).