Trial data for LYT-100, the deuterated form of pirfenidone, in healthy older adults

LYT-100 (deupirfenidone) is being used to treat inflammation and fibrosis, including idiopathic pulmonary fibrosis (IPF). It is a deuterated form of Pirfenidone designed to retain the beneficial pharmacology and clinically proven efficacy of pirfenidone and to have a highly differentiated pharmacokinetic (PK) profile. Multiple clinical studies in more than 400 patients have shown that this pharmacokinetic profile translates into good tolerability.

Pirfenidone is one of two standard treatments approved for idiopathic pulmonary fibrosis, the other beingnintedanib, both of which are effective but have significant tolerability issues. These tolerability issues lead to treatment interruptions and/or dose reductions below U.S. Food and Drug Administration (FDA)-approved doses, thereby limiting the effectiveness of these otherwise effective drugs. With dipirfenidone, it is designed to provide better outcomes for patients by enabling individuals to maintain the same or higher doses for longer periods of time.

The trial demonstrated that a dose of 550 mg of dipirfenidone (LYT-100) administered three times daily had bioequivalent drug exposure to the FDA-approved dose of pirfenidone of 801 mg three times daily. LYT-100 also has 24% lower peak drug concentrations than pirfenidone, a key factor often associated with tolerability. As previously reported, this dose also resulted in an approximately 50% reduction in gastrointestinal (GI) and central nervous system (CNS)-related adverse events (AEs) in subjects compared with subjects taking pirfenidone.

In addition, the data showed that the higher dose of LYT-100 (824 mg three times daily) achieved a 43% higher exposure level and was well tolerated, with no additional gastrointestinal or central nervous system adverse events occurring when titrated from LYT-100 550 mg three times daily in this trial, supporting the potential to provide enhanced efficacy in idiopathic pulmonary fibrosis that was well tolerated. This hypothesis is supported by phase 3 data with pirfenidone showing a dose-response effect on forced vital capacity and survival in patients with idiopathic pulmonary fibrosis.

Tolerability is a major challenge with currently available treatments for idiopathic pulmonary fibrosis, often leading to temporary and permanent dose reductions, premature discontinuation, and even patient reluctance to initiate treatment. The unique properties of dipirfenidone not only improve tolerability but also provide the opportunity to evaluate whether higher doses are associated with improved efficacy.

The original drug pirfenidone has been approved for marketing in China and has entered the scope of Class B medical insurance. Reimbursement is limited to patients who meet the indications. SpecificationsThe price of each box of 100mg*54 capsules is around RMB 500. There are also generic pirfenidone drugs produced in other countries overseas. For example, the price of a box of 200mg*30 tablets produced by an Indian pharmaceutical factory is around RMB 100 (the price may fluctuate due to the exchange rate). The ingredients of the generic drugs are basically the same as those of the original drug. For more drug information and specific prices, please consult Yaode Medical Consultant.