Thông tin thuốc gốc
Chỉ định và Liều dùng
Chronic hepatitis C
Adult: As combination therapy with antiviral treatment regimen in patients with chronic HCV genotype 1, 2, 3, or 4: 400 mg once daily. Treatment duration may vary depending on genotype and treatment regimen. Refer to detailed product guideline.
Child: As combination therapy with antiviral treatment regimen in patients with chronic HCV genotype 2 or 3: ≥12 years or weighing ≥35 kg: Same as adult dose.
Special Patient Group

CPIC guidelines identify IL28B also known as IFNL3 as the strongest baseline predictor of responses for previously untreated patients with HCV genotype 1. Since sofosbuvir is indicated as combination therapy with ribavirin and peginterferon-α, IFNL3 genotype may be considered relevant.

IFNL3 variation is the most established pretreatment predictor of therapy response. The two identified IFNL3 polymorphisms are rs12979860 and rs8099917. The alleles of these polymorphism are associated with increase sustained virological response (SVR) in HCV genotype 1 patients, specifically allele CC for rs12979860 and allele TT for rs8099917.

The allele frequency of rs12979860 varies among different ethnic backgrounds. The rs12979860 favorable C allele is most frequently found in East Asians, followed by Caucasians and Hispanics and least common among individuals of African origin.

CPIC states the following assignment and recommendations of probable IFNL3 phenotypes based on genotypes:

Favorable response genotype (carrier of 2 favorable response alleles e.g. rs12979860 CC)
Patient may have higher SVR rate to peginterferon-α and ribavirin therapy. Approx 70% chance for SVR after 48 weeks of therapy. Consider implications before starting peginterferon-α and ribavirin treatment.

Unfavorable response genotype (carrier of at least 1 unfavorable response alleles e.g. rs12979860 CT or TT)
Patient may have lower SVR rate to peginterferon-α and ribavirin therapy. Approx 30% chance for SVR after 48 weeks of therapy. Consider implication before starting peginterferon- α and ribavirin treatment.
Cách dùng
May be taken with or without food.
Chống chỉ định
Hypersensitivity. Pregnancy (when used in combination with ribavirin and peginterferon-α). Concomitant use with amiodarone and potent P-glycoprotein (P-gp) inducers.
Thận trọng
Patient with diabetes mellitus; co-infection with HIV; 1 or more factors associated with lower response rates to interferon-based therapies (e.g. advanced fibrosis/cirrhosis, high baseline viral concentration, black race, IL28B non-CC genotype, prior null response to peginterferon-α and ribavirin therapy). Patient awaiting liver transplantation and liver transplant recipients. Not intended for use as a monotherapy. Children. Hepatic impairment. Lactation.
Phản ứng phụ
Blood and lymphatic system disorders: Anaemia, neutropenia.
Gastrointestinal disorders: Nausea, decreased appetite, diarrhoea, vomiting, abdominal discomfort, constipation, dyspepsia, dry mouth.
General disorders and administration site conditions: Fatigue, flu-like symptoms, fever, irritability.
Hepatobiliary disorders: Increased blood bilirubin.
Metabolism and nutrition disorders: Decreased appetite and weight.
Musculoskeletal and connective tissue disorders: Asthenia, myalgia, arthralgia, muscle spasms, chills.
Nervous system disorders: Headache, migraine, memory impairment.
Psychiatric disorders: Insomnia, depression, anxiety, agitation.
Respiratory, thoracic and mediastinal disorders: Nasopharyngitis, dyspnoea, cough, dyspnoea exertional.
Skin and subcutaneous tissue disorders: Rash, pruritus, alopecia, dry skin.
Potentially Fatal: Hepatitis B virus reactivation.
PO: B, X (if used w/ ribavirin/peginterferon-α)
Thông tin tư vấn bệnh nhân
This drug may cause dizziness, blurred vision, and disturbance in attention, if affected, do not drive or operate machinery.
Monitor LFT, CBC, INR, calculated GFR, quantitative HCV viral load and HCV genotype at baseline within 12 weeks prior to starting the therapy. Monitor CBC, serum creatinine, calculated GFR during treatment; LFT (after 4 weeks of therapy and as necessary); quantitative HCV viral load (after 4 weeks of therapy then at 12 weeks after completion of treatment). Perform hepatitis B surface antigen (HBsAg) and hepatitis B core antibody (anti-HBc) prior to initiation of treatment. Monitor for clinical and laboratory signs of hepatitis flare or hepatitis B virus (HBV) reactivation in patients with serologic evidence of HBV infection during and post-treatment follow-up. Monitor changes in glucose tolerance and signs and symptoms of hypoglycaemia in diabetic patients.
Tương tác
May cause symptomatic hypoglycaemia when given with antidiabetic agents. May diminish anticoagulant effect of vitamin K antagonists (e.g. warfarin). May decrease concentration of sofosbuvir with modafinil, oxcarbazepine, rifapentine and HIV protease inhibitor (e.g. tipranavir/ritonavir) thereby reducing therapeutic effect.
Potentially Fatal: May cause severe symptomatic bradycardia and heart block when given with amiodarone. Significantly decreased plasma concentration with potent P-gp inducers (e.g. carbamazepine, phenytoin, phenobarbital).
Food Interaction
Decreased plasma concentration of sofosbuvir with St. John’s wort.
Tác dụng
Description: Sofosbuvir is a nucleotide analogue inhibitor, effective against hepatitis C virus (HCV) nonstructural 5B (NS5B) polymerase, which is necessary for viral replication. It is a direct-acting antiviral prodrug that has broad genotypic coverage and acts as chain terminator.
Absorption: Time to peak plasma concentration: Approx 0.5-2 hours.
Distribution: Plasma protein binding: Approx 61-65%.
Metabolism: Extensively metabolised in the liver via sequential hydrolysis, phosphoramidate cleavage followed by phosphorylation to form pharmacologically active nucleoside analogue triphosphate GS-461203, and subsequent dephosphorylation to form nucleoside inactive metabolite GS-331007.
Excretion: Mainly via urine (approx 80%; 78% as GS-331007 metabolite, 3.5 % as unchanged drug); faeces (approx 14%); expired air (approx 2.5%). Elimination half-life: 0.4 hour.
Đặc tính

Chemical Structure Image

Source: National Center for Biotechnology Information. PubChem Database. Sovaldi, CID=45375808, (accessed on Jan. 23, 2020)

Bảo quản
Store below 30°C.
Phân loại MIMS
Phân loại ATC
J05AP08 - sofosbuvir ; Belongs to the class of antivirals for treatment of HCV infections. Used in the treatment of hepatitis C viral infections.
Muir AJ, Gong L, Johnson SG, et al. Clinical Pharmacogenetics Implementation Consortium (CPIC) Guidelines for IFNL3 (IL28B) Genotype and PEG Interferon-α-Based Regimens. CPIC Guidelines. 2014 Feb;95(2):141-146. doi: 10.1038/clpt.2013.203. Accessed 15/10/2019

Anon. IL28B - Sofosbuvir (Pharmacogenomics). Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. Accessed 15/10/2019.

Anon. Sofosbuvir. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. Accessed 15/10/2019.

Buckingham R (ed). Sofosbuvir. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. Accessed 17/10/2019.

Clinical Annotation for rs12979860 (IFNL3, IFNL4); Ledispasvir or Sofosbuvir; Hepatitis C, Chronic (Level 3 Efficacy). Pharmacogenomics Knowledgebase (PharmGKB). Accessed 15/10/2019.

Clinical Annotation for rs8099917(IFNL3, IFNL4); Ledispasvir or Sofosbuvir; Hepatitis C, Chronic (Level 3 Efficacy). Pharmacogenomics Knowledgebase (PharmGKB). Accessed 15/10/2019.

Clinical Pharmacogenetics Implementation Consortium (CPIC) Guideline for IFNL3 (IL28B) Genotype and PEG Interferon-Alpha-Based Regimens. Clinical Pharmacogenetics Implementation Consortium (CPIC). Accessed 15/10/2019.

Joint Formulary Committee. Sofosbuvir. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. Accessed 17/10/2019.

Sovaldi Tablet, Film-Coated (Gilead Sciences, Inc.). DailyMed. Source: U.S. National Library of Medicine. Accessed 17/10/2019.

Thông báo miễn trừ trách nhiệm: Thông tin này được MIMS biên soạn một cách độc lập dựa trên thông tin của Sofosbuvir từ nhiều nguồn tài liệu tham khảo và được cung cấp chỉ cho mục đích tham khảo. Việc sử dụng điều trị và thông tin kê toa có thể khác nhau giữa các quốc gia. Vui lòng tham khảo thông tin sản phẩm trong MIMS để biết thông tin kê toa cụ thể đã qua phê duyệt ở quốc gia đó. Mặc dù đã rất nỗ lực để đảm bảo nội dung được chính xác nhưng MIMS sẽ không chịu trách nhiệm hoặc nghĩa vụ pháp lý cho bất kỳ yêu cầu bồi thường hay thiệt hại nào phát sinh do việc sử dụng hoặc sử dụng sai các thông tin ở đây, về nội dung thông tin hoặc về sự thiếu sót thông tin, hoặc về thông tin khác. © 2021 MIMS. Bản quyền thuộc về MIMS. Phát triển bởi
Register or sign in to continue
Asia's one-stop resource for medical news, clinical reference and education
Sign up for free
Already a member? Sign in