halofuginone

Action and Spectrum

Actions and spectrum: 

• Antiprotozoal Activity: halofuginone is primarily used to combat protozoan parasites, particularly as an antimalarial and anti-coccidial agent. 
• Antifibrotic Properties: It has shown promise in reducing tissue scarring and fibrosis, making it a potential treatment for fibrotic diseases. 
• Immunomodulation: halofuginone exhibits immunomodulatory effects, which means it can influence the immune system to manage inflammatory responses. 
• Anticancer Effects: Some research suggests that halofuginone may have anticancer properties, potentially inhibiting tumor growth and metastasis. 

Drug Interaction

Adverse Reaction

Frequency not defined 

Nausea 

vomiting

hepatic toxicity 

fatigue 

Black Box Warning

Black Box Warning: 

halofuginone does not typically carry a black box warning. 

Contraindication / Caution

Contraindication/Caution: 

Contraindication: 

• Hypersensitivity: Individuals who have a known hypersensitivity or allergy to halofuginone or any of its components should avoid using the medication. 
• Pregnancy and Lactation: The safety of halofuginone during pregnancy and breastfeeding has not been well established. It is usually not recommended for use during pregnancy or while breastfeeding unless the potential benefits outweigh the risks. 
• Children: halofuginone’s safety and efficacy in pediatric populations have not been extensively studied. Its use in children should be closely monitored and guided by a healthcare professional.

Caution: 

• Side Effects: Be cautious of potential side effects or adverse reactions associated with halofuginone use. If any unexpected or severe side effects occur, consult a healthcare professional promptly. 
• Dose and Duration: Use halofuginone according to the prescribed dose and duration. Avoid taking more than recommended or for a longer period without medical advice. 
• Liver Disease: halofuginone may undergo hepatic metabolism. Patients with pre-existing liver disease may need dosage adjustments or careful monitoring, as their liver function could impact the drug’s clearance and metabolism. 
• Kidney Disease: halofuginone may be excreted through the kidneys. Individuals with kidney impairment may need dosage adjustments or monitoring, as the drug’s excretion could be altered.

Comorbidities: 

• Immune System Disorders: Since halofuginone affects the immune response, individuals with immune system disorders, such as autoimmune diseases, should be cautious when considering its use. 
• Pediatric Patients: The safety and efficacy of halofuginone in pediatric populations may not be well-established. Special considerations and careful monitoring may be necessary when considering its use in children. 
• Neurological Conditions: Some individuals with neurological conditions may experience side effects like dizziness or drowsiness. Caution is advised if using halofuginone alongside these conditions. 

Pregnancy / Lactation

Pregnancy consideration: pregnancy category: not assigned 

Lactation: excreted into human milk: unknown  

Pregnancy category: 

• Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester. 
• Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 
• Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.   
• Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits. 
• Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women. 
• Category N: There is no data available for the drug under this category. 

Pharmacology

Pharmacology: 

halofuginone is a pharmacologically active compound that primarily acts as an inhibitor of an enzyme called ribosomal S6 kinase 1 (S6K1). This plays a major role in protein synthesis and cell proliferation. By inhibiting S6K1, halofuginone interferes with the process of collagen production and inhibits the growth of fibrotic tissue. This mechanism is relevant in the context of fibrotic and autoimmune diseases. halofuginone’s pharmacology makes it an intriguing candidate for the treatment of conditions where uncontrolled tissue fibrosis or immune system dysfunction is a concern.  

Pharmacodynamics: 

• Anti-Fibrotic Effects: halofuginone interferes with the synthesis of collagen, a protein responsible for fibrotic tissue formation. This makes it a valuable agent in preventing or reducing fibrosis in conditions such as systemic sclerosis, pulmonary fibrosis, and liver fibrosis. 
• Immunomodulation: halofuginone can regulate immune responses by influencing the differentiation of immune cells. This immunomodulatory effect is explored in the context of autoimmune diseases. 
• Anti-Angiogenesis: halofuginone has been shown to inhibit the formation of new blood vessels. This is important in the context of cancer therapy, where restricting blood supply to tumors can impede their growth.

Pharmacokinetics: 

Absorption 

halofuginone is typically administered orally, and its absorption occurs in the gastrointestinal tract. 

Distribution 

halofuginone primarily binds to plasma proteins, particularly albumin. 

Metabolism 

halofuginone undergoes extensive metabolism in the liver through the cytochrome P450 enzyme system, particularly CYP3A4. It is converted into several metabolites. 

Elimination and excretion 

The metabolites of halofuginone are primarily eliminated through the feces. 

Adminstartion

Administration: 

• Dosage: The dosage of halofuginone can vary depending on the condition being treated. Follow your healthcare provider’s recommendations and the instructions on the prescription label. 
• Timing: halofuginone is usually taken with food or shortly after a meal to improve absorption and reduce the risk of stomach upset. 
• Consistency: Try to take halofuginone at the same time each day to maintain consistent drug levels in your system. 
• Duration: Continue taking halofuginone for the full course of treatment, even if your symptoms improve. Do not discontinue the medication without consulting your healthcare provider. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: halofuginone 

Pronounced: (hal-oh-foo-gi-none)  

Why do we use halofuginone? 

halofuginone has demonstrated activity against the Plasmodium parasite, which causes malaria. It may be used in combination with other antimalarial drugs for the treatment of malaria infections. halofuginone has been investigated for its potential to reduce fibrosis. It may be used in research and clinical trials for fibrotic conditions, such as idiopathic pulmonary fibrosis and liver fibrosis. Some studies have explored the potential use of halofuginone in the treatment of IBD, including Crohn’s disease & ulcerative colitis, due to its anti-inflammatory effects.