Pulfibro 801 mg Tablet

Pulfibro 801 mg is indicated in adults for the treatment of mild to moderate Idiopathic Pulmonary Fibrosis (IPF).

Immunosuppressant

Pulfibro 801 mg is an orally active, small molecule that shows a wide range of biologic activity. In vitro evidence has shown that Pulfibro 801 mg inhibits collagen synthesis, down-regulates profibrotic cytokines and decreases fibroblast proliferation. Pulfibro 801 mg leads to a reduction of TGF-beta2 mRNA levels and of the mature TGF-beta2 protein due to decreased expression and direct inhibition of the TGF-beta pro-protein convertase furin. In addition, Pulfibro 801 mg reduces the protein levels of the matrix metalloproteinase (MMP)-11, a TGF-beta target gene and furin substrate involved in carcinogenesis.

Treatment with Pulfibro 801 mg should be initiated and supervised by specialist physicians experienced in the diagnosis and treatment of IPF. Upon initiating treatment, the dose should be titrated to the recommended daily dose of nine 267 mg tablets or one 801 mg tablet per day over a 14-days period for adult as follows: Days 1 to 7: One 267 mg tablet administered three times a day (801 mg/day) Days 8 to 14: One 534 mg tablets administered three times a day (1602 mg/day) Day 15 onward: Three 267 mg tablets or one 801 mg tablet administered three times a day (2403 mg/day) The recommended daily dose of Pulfibro 801 mg for patients with IPF is three 267 mg tablets or one 801 mg three times a day with food for a total of 2403 mg/day. Doses above 2403 mg/day are not recommended for any patient. Patients who miss 14 consecutive days or more of Pulfibro 801 mg treatment should re-initiate therapy by undergoing the initial 2-week titration regimen up to the recommended daily dose. For treatment interruption of less than 14 consecutive days, the dose can be resumed at the previous recommended daily dose without titration.Dose adjustments and other considerations for safe use: Gastrointestinal events: In patients who experience intolerance to therapy due to gastrointestinal side effects, patients should be reminded to take the medicinal product with food. If symptoms persist Pulfibro 801 mg may be reduced to 1-2 capsules (267 mg-534 mg) 2-3 times/day with food with re-escalation to the recommended daily dose as tolerated. If symptoms continue, patients may be instructed to interrupt treatment for 1 to 2 weeks to allow symptoms to resolve.Photosensitivity reaction or rash: Patients who experience a mild to moderate photosensitivity reaction or rash should be reminded of the instruction to use a sunblock daily and to avoid sun exposure. The dose of Pulfibro 801 mg may be reduced to 3 capsules/day (1 capsule three times a day). If the rash persists after 7 days, Pulfibro 801 mg should be discontinued for 15 days, with re-escalation to the recommended daily dose in the same manner as the dose escalation period. Patients who experience severe photosensitivity reaction or rash should be instructed to interrupt the dose and to seek medical advice. Once the rash has resolved, Pulfibro 801 mg may be re-introduced and re-escalated up to the recommended daily dose at the discretion of the physician.Hepatic function: In the event of significant elevation of alanine and/or aspartate aminotransferases (ALT/AST) with or without bilirubin elevation, the dose of Pulfibro 801 mg should be adjusted or treatment discontinued according to the guidelines.

Route of administration: Pulfibro 801 mg is administered orally with food.Adults: Upon initiating treatment, the dose should be titrated to the recommended daily dose of nine 267 mg tablets or three 801 mg tablet per day over a 14-days period as follows: Days 1 to 7: One 267 mg tablet administered three times a day (801 mg/day) Days 8 to 14: Two 267 mg tablets administered three times a day (1602 mg/day) Day 15 onward: Three 267 mg tablets or one 801 mg tablet administered three times a day (2403 mg/day) The recommended daily dose of Pulfibro 801 mg for patients with IPF is three 267 mg tablets or one 801 mg three times a day with food for a total of 2403 mg/day. Doses above 2403 mg/day are not recommended for any patient. Patients who miss 14 consecutive days or more of Pulfibro 801 mg treatment should re-initiate therapy by undergoing the initial 2-week titration regimen up to the recommended daily dose. For treatment interruption of less than 14 consecutive days, the dose can be resumed at the previous recommended daily dose without titration. Dose adjustments and other considerations for safe use: Gastrointestinal events: In patients who experience intolerance to therapy due to gastrointestinal side effects, patients should be reminded to take the medicinal product with food. If symptoms persist Pulfibro 801 mg may be reduced to 1-2 tablets (267 mg-534 mg) 2-3 times/day with food with re-escalation to the recommended daily dose as tolerated. If symptoms continue, patients may be instructed to interrupt treatment for 1 to 2 weeks to allow symptoms to resolve. Photosensitivity reaction or rash: Patients who experience a mild to moderate photosensitivity reaction or rash should be reminded of the instruction to use a sunblock daily and to avoid sun exposure. The dose of Pulfibro 801 mg may be reduced to three 267 mg tablets/day (one 267 mg tablet three times a day). If the rash persists after 7 days, Pulfibro 801 mg should be discontinued for 15 days, with re-escalation to the recommended daily dose in the same manner as the dose escalation period. Patients who experience severe photosensitivity reaction or rash should be instructed to interrupt the dose and to seek medical advice. Once the rash has resolved, Pulfibro 801 mg may be re-introduced and re-escalated up to the recommended daily dose at the discretion of the physician. Hepatic function: In the event of significant elevation of alanine and/or aspartate aminotransferases (ALT/AST) with or without bilirubin elevation, the dose of Pulfibro 801 mg should be adjusted or treatment discontinued according to the guidelines.

With medicine: Moderate (e.g., ciprofloxacin) and strong inhibitors of CYP1A2 (e.g., fluvoxamine) increase the systemic exposure of Pulfibro 801 mg and may alter the adverse reaction profile of Pulfibro 801 mg. Discontinue fluvoxamine prior to administration of Pulfibro 801 mg or reduce to 267 mg three times a day. Consider dosage reduction with use of ciprofloxacin.With food and others: None. A reduced incidence of adverse reactions was observed in the fed group when compared to the fasted group.

Hypersensitivity to the active substance or to any of the excipients, concomitant use of fluvoxamine, severe hepatic impairment or end stage liver disease, severe renal impairment (CrCl <30 ml/min) or end stage renal disease requiring dialysis.

Common: nausea, rash, abdominal pain, upper respiratory tract infection, diarrhea, fatigue, headache, dyspepsia, dizziness, vomiting, anorexia, gastroesophageal reflux disease, sinusitis, insomnia, weight decrease, and arthralgia.Rare: photosensitivity reaction, decreased appetite, pruritus, asthenia, dysgeusia, and non-cardiac chest pain.

Pregnancy: There are no data from the use of Pulfibro 801 mg in pregnant women. In animals placental transfer of Pulfibro 801 mg and/or its metabolites occurs with the potential for accumulation of Pulfibro 801 mg and/or its metabolites in amniotic fluid. At high doses (1000 mg/kg/day) rats exhibited prolongation of gestation and reduction in fetal viability. As a precautionary measure, it is preferable to avoid the use of Pulfibro 801 mg during pregnancy.Lactation: It is unknown whether Pulfibro 801 mg or its metabolites are excreted in human milk. Available pharmacokinetic data in animals have shown excretion of Pulfibro 801 mg and/or its metabolites in milk with the potential for accumulation of Pulfibro 801 mg and/or its metabolites in milk. A risk to the suckling child cannot be excluded. A decision must be made whether to discontinue breast-feeding or to discontinue from Pulfibro 801 mg therapy, taking into account the benefit of breast-feeding for the child and the benefit of Pulfibro 801 mg therapy for the mother.Fertility: No adverse effects on fertility were observed in preclinical studies. Effects on ability to drive and use machines: No studies on the effects of the ability to drive and use machines have been performed. Pulfibro 801 mg may cause dizziness and fatigue, which could influence the ability to drive or use machines.

Elevated liver enzymes: ALT, AST, and bilirubin elevations have occurred with Pulfibro 801 mg. Monitor ALT, AST, and bilirubin before and during treatment. Temporary dosage reductions or discontinuations may be required. Photosensitivity and rash: Photosensitivity and rash have been noted with Pulfibro 801 mg. Avoid exposure to sunlight and sunlamps. Wear sunscreen and protective clothing daily. Temporary dosage reductions or discontinuations may be required. Gastrointestinal disorders: Nausea, vomiting, diarrhea, dyspepsia, gastroesophageal reflux disease, andabdominal pain have occurred with Pulfibro 801 mg. Temporary dosage reductions or discontinuations may be required.

There is limited clinical experience with overdose. Multiple doses of Pulfibro 801 mg up to a dose of 4806 mg/day were administered as six 267 mg tablets three times daily to healthy adult volunteers over a 12-day dose escalation period. Adverse reactions were mild, transient, and consistent with the most frequently reported adverse reactions for Pulfibro 801 mg.

Store in a cool & dry place. Protect from light & moisture. Keep all medicine out of reach of children.

Immunosuppressant

Pulfibro 801 mg is a novel agent with anti-inflammatory, antioxidant, and anti-fibrotic properties. It may improve lung function and reduce the number of acute exacerbations in patients with idiopathic pulmonary fibrosis (IPF). The precise mechanism of action of Pulfibro 801 mg and its specific molecular targets have yet to be elucidated. One vital anti-fibrotic mechanism involves the suppression of TGF-β1 (transforming growth factor-β1), a key cytokine involved in fibrogenesis and extracellular matrix production. There is also evidence to suggest that Pulfibro 801 mg has the ability to downregulate the expression of potent pro-inflammatory cytokines including TNF-α, interleukin-1, and interferon-gamma. In animal models, Pulfibro 801 mg can inhibit both the influx of inflammatory cells and the increased pulmonary vascular permeability induced by bleomycin.

Pregnancy: There are no data from the use of Pulfibro 801 mg in pregnant women. In animals’ placental transfer of Pulfibro 801 mg and/or its metabolites occurs with the potential for accumulation of Pulfibro 801 mg and/or its metabolites in amniotic fluid. At high doses (1000 mg/kg/day) rats exhibited prolongation of gestation and reduction in fetal viability. As a precautionary measure, it is preferable to avoid the use of Pulfibro 801 mg during pregnancy.Lactation: It is unknown whether Pulfibro 801 mg or its metabolites are excreted in human milk. Available pharmacokinetic data in animals have shown excretion of Pulfibro 801 mg and/or its metabolites in milk with the potential for accumulation of Pulfibro 801 mg and/or its metabolites in milk. A risk to the suckling child cannot be excluded. A decision must be made whether to discontinue breast-feeding or to discontinue from Pulfibro 801 mg therapy, taking into account the benefit of breast-feeding for the child and the benefit of Pulfibro 801 mg therapy for the mother.Fertility: Pulfibro 801 mg had no effects on fertility and reproductive performance in rats at dosages up to 1000 mg/kg/day (approximately 3 times the MRDD in adults on mg/m2 basis)

Use in Children & Adolescents: It is not known if Pulfibro 801 mg is safe and effective in children & adolescents.Hepatic Impairment: Monitor for adverse reactions and consider dosage modification or discontinuation of Pulfibro 801 mg as needed. Pulfibro 801 mg is not recommended for use in patients with severe hepatic impairment.Renal Impairment: Monitor for adverse reactions and consider dosage modification or discontinuation of Pulfibro 801 mg as needed. Pulfibro 801 mg is not recommended for use in patients with end-stage renal disease on dialysis.Smokers: Decreased exposure has been noted in smokers which may alter the efficacy profile of Pulfibro 801 mg.