Tenofovir Disoproxil Fumarate 300 mg Tablet, Film Coated, 30-count
🆔 Identity & classification
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🏷️ RxNorm drug class
This medicine belongs to the Nucleoside and nucleotide reverse transcriptase inhibitors class.
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🏭 Manufacturer & labeler
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🩺 Clinical
Tenofovir alafenamide (AF) is used to treat chronic (long term) hepatitis B virus (HBV) infection. Tenofovir is in a class of medications called nucleoside reverse transcriptase inhibitors (NRTIs). It works by decreasing the amount of HBV in the blood. Tenofovir AF will not cure hepatitis B and may not prevent complications of chronic hepatitis B. Tenofovir AF may not prevent the spread of hepatitis B to other people.
Read the full MedlinePlus article ↗Patient education
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💊 What it looks like
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🧪 Inactive Ingredients / Excipients
Inactive ingredients, also called excipients, are components of the drug product other than the active ingredient. They may include fillers, dyes, coatings, preservatives, flavors, or other formulation ingredients.
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UNII OP1R32D61U
Microcrystalline cellulose is a purified form of cellulose, a natural fiber from plant sources. It acts as a binder and filler in tablets and capsules, helping hold ingredients together and give the medicine its shape and size.
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UNII M28OL1HH48
Croscarmellose sodium is a plant-based substance derived from cellulose. It acts as a disintegrant, helping tablets and capsules break down quickly in the digestive system so the medicine can be absorbed.
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UNII 3NXW29V3WO
Hypromellose is a plant-based thickener made from cellulose. It's used in medicines as a binder to hold ingredients together, a coating for tablets, and a thickener for liquids.
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UNII EWQ57Q8I5X
Lactose monohydrate is a natural sugar derived from milk. It serves as a filler and binder in tablets and capsules, helping create the proper size, texture, and consistency of the medicine.
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UNII 70097M6I30
Magnesium stearate is a salt made from magnesium and stearic acid, a fatty substance. It's used in tablets and capsules as a lubricant and glidant to help ingredients flow smoothly during manufacturing and prevent sticking.
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UNII O8232NY3SJ
A plant-based carbohydrate derived from corn kernels. It acts as a filler to add bulk, a binder to hold ingredients together, and a disintegrant to help the tablet break apart in your stomach for absorption.
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UNII 15FIX9V2JP
Titanium dioxide is a bright white mineral powder commonly used as a colorant and opacifying agent. It makes pills and tablets white or lighter in color and helps make coatings non-transparent.
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UNII XHX3C3X673
Triacetin is a clear, oily liquid made from glycerin and acetic acid. It works as a plasticizer and solvent in medicines, helping soften coatings and improve how liquids mix together in formulations.
8 inactive ingredients listed in the exact product block matched to this NDC.
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ingredient classCode="IACT" elements from the exact product block matched by this NDC. Label-section narrative from DailyMed / the openFDA label index is shown separately when available.Inactive ingredient FAQ
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💲 Pricing
A drug doesn't have one price. Each row is a different public payment system, and none is what you'd pay at the counter — that depends on your insurance. The ⓘ on each row explains what it measures.
| Price system | Per ea | Per package |
|---|---|---|
| Retail pharmacies payNADAC · weekly | $0.311 | $9.33 / 30 tablets |
| Medicaid paysCMS SDUD · 12 mo | $1.09 | $32.83 / 30 tablets |
| Medicare drug plans payPart D · Q2 2026 | $1.04 | $31.29 / 30 tablets |
Where does this data come from?
🔁 Therapeutic equivalents
| Product | Labeler | Pack | NADAC/unit | TE | Status | Price vs. this |
|---|---|---|---|---|---|---|
| tenofovir disoproxil fumarate 300 mg 00904-6821-04 | Major | 30 tablets | $0.311 | AB | Availability likely | — |
| Tenofovir Disoproxil Fumarate 300 mgthis 16714-0820-01 | NorthStar | 30 tablets | $0.311 | AB | Availability likely | — |
| tenofovir disoproxil fumarate 300 mg 33342-0096-07 | Macleods | 30 tablets | $0.311 | AB | Availability likely | — |
| Tenofovir Disoproxil Fumarate 300 mg 50268-0758-12 | AvPAK | 20 tablets | $0.311 | AB | Availability likely | — |
| Tenofovir Disoproxil Fumarate 300 mg 62135-0466-30 | Chartwell | 30 tablets | $0.311 | AB | Availability likely | — |
| Tenofovir Disoproxil Fumarate 300 mg 64380-0714-04 | Strides | 30 tablets | $0.311 | AB | Availability likely | — |
| Tenofovir Disoproxil Fumarate 300 mg 65862-0421-30 | Aurobindo | 30 tablets | $0.311 | — | Availability likely | — |
| Tenofovir Disoproxil Fumarate 300 mg 69076-0105-03 | Quinn | 30 tablets | $0.311 | AB | Availability likely | — |
| Tenofovir disoproxil fumarate 300 mg 69097-0533-02 | Cipla | 30 tablets | $0.311 | AB | Availability likely | — |
| Tenofovir Disoproxil Fumarate 300 mg 71921-0105-33 | Florida | 30 tablets | $0.311 | AB | Availability likely | — |
| Viread 300 mg 61958-0401-01 | Gilead | 30 tablets | $40.728 | AB | Availability likely | +12995% |
| Tenofovir Disoproxil Fumarate 300 mg 31722-0535-01 | Camber | 100 tablets | — | AB | FDA listed | — |
| Tenofovir Disoproxil Fumarate 300 mg 42291-0800-30 | AvKARE | 30 tablets | — | AB | FDA listed | — |
| Tenofovir Disoproxil Fumarate 300 mg 50090-7202-00 | A-S | 30 tablets | — | AB | FDA listed | — |
| Tenofovir Disoproxil Fumarate 300 mg 63629-9729-01 | Bryant | 30 tablets | — | AB | FDA listed | — |
| Tenofovir Disoproxil Fumarate 300 mg 71335-2364-01 | Bryant | 30 tablets | — | AB | FDA listed | — |
| Tenofovir Disoproxil Fumarate 300 mg 72789-0361-07 | PD-Rx | 7 tablets | — | AB | FDA listed | — |
| Tenofovir Disoproxil Fumarate 300 mg 71335-3155-01 | Bryant | 30 tablets | — | AB | FDA listed | — |
Where does this data come from?
⏳ Availability & generic status
This product is an FDA-approved generic. Other versions of the same drug are listed under Therapeutic equivalents, least expensive first.
Where does this data come from?
🗺️ Medicaid utilization & spend
📊 Medicare Part D spend CMS · PART D · 2026 (Q1)
🔬 Reported adverse events (FAERS)
Top reported reactions
Age at onset
Reporter sex
Serious outcomes
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📦 Packaging — all sizes for this product
| Package NDC | Description | Marketing start | Status |
|---|---|---|---|
| 16714-0820-01 You're viewing this | 30 TABLET, FILM COATED in 1 BOTTLE (16714-820-01) | 2018-11-12 | Active |
📄 Full prescribing information FDA SPL
🚨 Boxed Warning ▾
BOXED WARNING WARNING: POSTTREATMENT EXACERBATION OF HEPATITIS Severe acute exacerbations of hepatitis have been reported in HBV-infected patients who have discontinued anti-hepatitis B therapy, including tenofovir disoproxil fumarate tablets. Hepatic function should be monitored closely with both clinical and laboratory follow-up for at least several months in patients who discontinue anti-hepatitis B therapy, including tenofovir disoproxil fumarate tablets. If appropriate, resumption of anti-hepatitis B therapy may be warranted [See Warnings and Precautions ( 5.1 )].
WARNING: POSTTREATMENT EXACERBATION OF HEPATITIS See full prescribing information for complete boxed warning. Severe acute exacerbations of hepatitis have been reported in HBV-infected patients who have discontinued anti-hepatitis B therapy, including tenofovir disoproxil fumarate tablets. Hepatic function should be monitored closely in these patients.
If appropriate, resumption of anti-hepatitis B therapy may be warranted. (5.1)
🎯 Indications and Usage ▾
1 INDICATIONS & USAGE Tenofovir disoproxil fumarate tablets are a nucleotide analog HIV-1 reverse transcriptase inhibitor and an HBV reverse transcriptase inhibitor. • Tenofovir disoproxil fumarate tablets are indicated in combination with other antiretroviral agents for the treatment of HIV-1 infection in adults and pediatric patients 2 years of age and older. (1) • Tenofovir disoproxil fumarate tablets are indicated for the treatment of chronic hepatitis B in adults and pediatric patients 12 years of age and older.
(1)
1.1HIV-1 Infection Tenofovir disoproxil fumarate tablets are indicated in combination with other antiretroviral agents for the treatment of HIV-1 infection in adults and pediatric patients 2 years of age and older. The following points should be considered when initiating therapy with tenofovir disoproxil fumarate tablets for the treatment of HIV-1 infection: • Tenofovir disoproxil fumarate tablets should not be used in combination with ATRIPLA ® , BIKTARVY ® , COMPLERA ® , DESCOVY ® , GENVOYA ® , ODEFSEY ® , STRIBILD ® , TRUVADA ® , or VEMLIDY ® [See Warnings and Precautions (5.4)].
1.2Chronic Hepatitis B Tenofovir disoproxil fumarate tablets are indicated for the treatment of chronic hepatitis B in adults and pediatric patients 12 years of age and older. The following points should be considered when initiating therapy with tenofovir disoproxil fumarate tablets for the treatment of chronic hepatitis B infection: • The indication in adults is based on safety and efficacy data from treatment of subjects who were nucleoside-treatment-naïve and subjects who were treatment-experienced with documented resistance to lamivudine.
Subjects were adults with HBeAg-positive and HBeAg-negative chronic hepatitis B with compensated liver disease [See Clinical Studies (14.2)]. • Tenofovir disoproxil fumarate tablets were evaluated in a limited number of subjects with chronic hepatitis B and decompensated liver disease [See Adverse Reactions (6.1), Clinical Studies (14.2)]. • The numbers of subjects in clinical trials who had adefovir resistance-associated substitutions at baseline were too small to reach conclusions of efficacy [See Microbiology (12.4), Clinical Studies ( 14.2)].
⏱️ Dosage and Administration ▾
2 DOSAGE & ADMINISTRATION • Recommended dose for the treatment of HIV-1 or chronic hepatitis B in adults and pediatric patients 12 years of age and older (35 kg or more): 300 mg once daily taken orally without regard to food. (2.1) • Recommended dose for the treatment of HIV-1 in pediatric patients (2 to less than 12 years of age): o Tablets: For pediatric patients weighing greater than or equal to 17 kg who can swallow an intact tablet, one tenofovir disoproxil fumarate tablet (300 mg based on body weight) once daily taken orally without regard to food.
(2.2) • Dose recommended in renal impairment in adults: o Creatinine clearance 30 to 49 mL/min: 300 mg every 48 hours. (2.3) o Creatinine clearance 10 to 29 mL/min: 300 mg every 72 to 96 hours. (2.3) o Hemodialysis: 300 mg every 7 days or after approximately 12 hours of dialysis.
(2.3)
2.1Recommended Dose in Adults and Pediatric Patients 12 Years of Age and Older (35 kg or more) For the treatment of HIV-1 or chronic hepatitis B: The dose is one 300 mg tenofovir disoproxil fumarate tablet once daily taken orally, without regard to food. In the treatment of chronic hepatitis B, the optimal duration of treatment is unknown. Safety and efficacy in pediatric patients with chronic hepatitis B weighing less than 35 kg have not been established.
2.2Recommended Dose in Pediatric Patients 2 Years to Less than 12 Years of Age HIV-1 Infection For the treatment of HIV-1 in pediatric patients 2 years of age and older, the recommended oral dose of tenofovir disoproxil fumarate tablet is 8 mg of tenofovir disoproxil fumarate (tenofovir DF) per kilogram of body weight (up to a maximum of 300 mg) once daily administered as tablets. Tenofovir disoproxil fumarate is available as tablets in 300 mg strength for pediatric patients who weigh greater than or equal to 17 kg and who are able to reliably swallow intact tablets.
The dose is one tablet once daily taken orally, without regard to food. Table 2 contain dosing recommendations for tenofovir disoproxil fumarate tablets based on body weight. Weight should be monitored periodically and the tenofovir disoproxil fumarate tablets dose adjusted accordingly.
Table 2 Dosing Recommendations for Pediatric Patients 2 Years of Age and Older and Weighing At Least 17 kg Using Tenofovir Disoproxil Fumarate Tablets Body Weight Kilogram (kg) Tablets Once Daily 17 to less than 22 150 mg 22 to less than 28 200 mg 28 to less than 35 250 mg 35 or greater 300 mg Chronic Hepatitis B Safety and efficacy of tenofovir disoproxil fumarate tablets in patients younger than 12 years of age have not been established.
2.3Dose Adjustment for Renal Impairment in Adults Significantly increased drug exposures occurred when tenofovir disoproxil fumarate tablets were administered to subjects with moderate to severe renal impairment [See Clinical Pharmacology (12.3)] . Therefore, the dosing interval of tenofovir disoproxil fumarate tablets 300 mg should be adjusted in patients with baseline creatinine clearance below 50 mL/min using the recommendations in Table 3. These dosing interval recommendations are based on modeling of single-dose pharmacokinetic data in non-HIV and non-HBV infected subjects with varying degrees of renal impairment, including end-stage renal disease requiring hemodialysis.
The safety and effectiveness of these dosing interval adjustment recommendations have not been clinically evaluated in patients with moderate or severe renal impairment; therefore, clinical response to treatment and renal function should be closely monitored in these patients [See Warnings and Precautions (5.2)] . No dose adjustment of tenofovir disoproxil fumarate tablets 300 mg is necessary for patients with mild renal impairment (creatinine clearance 50 to 80 mL/min). Routine monitoring of estimated creatinine clearance, serum phosphorus, urine glucose, and urine protein should be performed in patients with mild renal impairment [See Warnings and Precautions (5.2)] .
Table 3 Dosage Adj…
💊 Dosage Forms and Strengths ▾
3 DOSAGE FORMS & STRENGTHS Tenofovir disoproxil fumarate is available as tablets. Tenofovir disoproxil fumarate tablets contain 300 mg of tenofovir disoproxil fumarate, which is equivalent to 245 mg of tenofovir disoproxil. The tablets are white, almond shaped, film coated debossed with ‘H’ on one side and ‘123’ on other side. • Tablets: 300 mg ( 3 )
⛔ Contraindications ▾
4 CONTRAINDICATIONS None. None. (4)
⚠️ Warnings and Cautions ▾
5 WARNINGS AND PRECAUTIONS • New onset or worsening renal impairment: Can include acute renal failure and Fanconi syndrome. Assess estimated creatinine clearance before initiating treatment with tenofovir disoproxil fumarate tablets. In patients at risk for renal dysfunction, assess estimated creatinine clearance, serum phosphorus, urine glucose, and urine protein before initiating treatment with tenofovir disoproxil fumarate tablets and periodically during treatment.
Avoid administering tenofovir disoproxil fumarate tablets with concurrentor recent use of nephrotoxic drugs. (5.2) • Lactic acidosis/severe hepatomegaly with steatosis: Discontinue treatment in patients who develop symptoms or laboratory findings suggestive of lactic acidosis or pronounced hepatotoxicity. (5.3) • Coadministration with other products: Do not use with other tenofovir-containing products (e.g., ATRIPLA, BIKTARVY, COMPLERA, DESCOVY, GENVOYA, ODEFSEY, STRIBILD, TRUVADA, or VEMLIDY).
Do not administer in combination with HEPSERA. (5.4) • HIV testing: HIV antibody testing should be offered to all HBV-infected patients before initiating therapy with tenofovir disoproxil fumarate tablets. Tenofovir disoproxil fumarate tablets should only be used as part of an appropriate antiretroviral combination regimen in HIV-infected patients with or without HBV coinfection.
(5.5) • Decreases in bone mineral density (BMD): Consider assessment of BMD in patients with a history of pathologic fracture or other risk factors for osteoporosis or bone loss. (5.6) • Immune reconstitution syndrome: Observed in HIV-infected patients. May necessitate further evaluation and treatment.
(5.7) • Triple nucleoside-only regimens: Early virologic failure has been reported in HIV-infected patients. Monitor carefully and consider treatment modification. (5.8)
5.1Exacerbation of Hepatitis after Discontinuation of Treatment Discontinuation of anti-HBV therapy, including tenofovir disoproxil fumarate tablets, may be associated with severe acute exacerbations of hepatitis. Patients infected with HBV who discontinue tenofovir disoproxil fumarate tablets should be closely monitored with both clinical and laboratory follow-up for at least several months after stopping treatment. If appropriate, resumption of anti-hepatitis B therapy may be warranted.
5.2New Onset or Worsening Renal Impairment Tenofovir is principally eliminated by the kidney. Renal impairment, including cases of acute renal failure and Fanconi syndrome (renal tubular injury with severe hypophosphatemia), has been reported with the use of tenofovir disoproxil fumarate tablets [See Adverse Reactions (6.2)]. It is recommended that estimated creatinine clearance be assessed in all patients prior to initiating therapy and as clinically appropriate during therapy with tenofovir disoproxil fumarate tablets.
In patients at risk of renal dysfunction, including patients who have previously experienced renal events while receiving HEPSERA ®, it is recommended that estimated creatinine clearance, serum phosphorus, urine glucose, and urine protein be assessed prior to initiation of tenofovir disoproxil fumarate tablets, and periodically during tenofovir disoproxil fumarate tablets therapy. Dosing interval adjustment of tenofovir disoproxil fumarate tablets and close monitoring of renal function are recommended in all patients with creatinine clearance below 50 mL/min [See Dosage and Administration (2.3)].
No safety or efficacy data are available in patients with renal impairment who received tenofovir disoproxil fumarate tablets using these dosing guidelines, so the potential benefit of tenofovir disoproxil fumarate tablets therapy should be assessed against the potential risk of renal toxicity. Tenofovir disoproxil fumarate tablets should be avoided with concurrent or recent use of a nephrotoxic agent (e.g., high-dose or multiple non-steroidal anti-inflammatory drugs (NSAIDs)) [See Drug Interactions (7.1)]. Cases of acute renal failure a…
🤒 Adverse Reactions ▾
6 ADVERSE REACTIONS The following adverse reactions are discussed in other sections of the labeling: • Severe Acute Exacerbation of Hepatitis [See Boxed Warning, Warnings and Precautions ( 5.1 )]. • New Onset or Worsening Renal Impairment [See Warnings and Precautions ( 5.2 )]. • Lactic Acidosis/Severe Hepatomegaly with Steatosis [See Warnings and Precautions ( 5.3 )]. • Bone Effects [See Warnings and Precautions ( 5.6 )]. • Immune Reconstitution Syndrome [See Warnings and Precautions ( 5.7)]. • In HIV-infected adult subjects: Most common adverse reactions (incidence greater than or equal to 10%, Grades 2 to 4) are rash, diarrhea, headache, pain, depression, asthenia, and nausea.
(6.1) • In HBV-infected subjects with compensated liver disease: Most common adverse reaction (all grades) was nausea (9%). (6.1) • In pediatric subjects: Adverse reactions in pediatric subjects were consistent with those observed in adults. (6.1) • In HBV-infected subjects with decompensated liver disease: Most common adverse reactions (incidence greater than or equal to 10%, all grades) were abdominal pain, nausea, insomnia, pruritus, vomiting, dizziness, and pyrexia.
(6.1) To report SUSPECTED ADVERSE REACTIONS, contact NorthStar Rx LLC at 1-800-206-7821 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch
6.1Adverse Reactions from Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. Clinical Trials in Adult Patients with HIV-1 Infection More than 12,000 subjects have been treated with tenofovir disoproxil fumarate tablets alone or in combination with other antiretroviral medicinal products for periods of 28 days to 215 weeks in clinical trials and expanded access programs.
A total of 1,544 subjects have received tenofovir disoproxil fumarate tablets 300 mg once daily in clinical trials; over 11,000 subjects have received tenofovir disoproxil fumarate tablets in expanded access programs. The most common adverse reactions (incidence greater than or equal to 10%, Grades 2 to 4) identified from any of the 3 large controlled clinical trials include rash, diarrhea, headache, pain, depression, asthenia, and nausea. Treatment-Naïve Patients Study 903 - Treatment-Emergent Adverse-Reactions: The most common adverse reactions seen in a double-blind comparative controlled trial in which 600 treatment-naïve subjects received tenofovir disoproxil fumarate tablets (N=299) or stavudine (N=301) in combination with lamivudine and efavirenz for 144 weeks (Study 903) were mild to moderate gastrointestinal events and dizziness.
Mild adverse reactions (Grade 1) were common with a similar incidence in both arms and included dizziness, diarrhea, and nausea. Selected treatment-emergent moderate to severe adverse reactions are summarized in Table 4. Table 4 Selected Treatment-Emergent Adverse Reactionsa (Grades 2 to 4) Reported in ≥5% in Any Treatment Group in Study 903 (0 to 144 Weeks) Tenofovir disoproxil fumarate Tablets +3TC+EFV d4T+3TC+EFV N=299 N=301 Body as a Whole Headache Pain Fever Abdominal pain Back pain Asthenia 14% 13% 8% 7% 9% 6% 17% 12% 7% 12% 8% 7% Digestive System Diarrhea Nausea Dyspepsia Vomiting 11% 8% 4% 5% 13% 9% 5% 9% Metabolic Disorders Lipodystrophy b 1% 8% Musculoskeletal Arthralgia Myalgia 5% 3% 7% 5% Nervous System Depression Insomnia Dizziness Peripheral neuropathy c Anxiety 11% 5% 3% 1% 6% 10% 8% 6% 5% 6% Respiratory Pneumonia 5% 5% Skin and Appendages Rash event d 18% 12% a.
Frequencies of adverse reactions are based on all treatment-emergent adverse events, regardless of relationship to study drug. b. Lipodystrophy represents a variety of investigator-described adverse events not a protocol-defined syndrome. c. Peripheral neuropathy includes peripheral neuritis and neuropathy. d.
Rash event includes rash, pruri…
🔄 Drug Interactions ▾
7 DRUG INTERACTIONS This section describes clinically relevant drug interactions with tenofovir disoproxil fumarate tablets. Drug interactions trials are described elsewhere in the labeling [See Clinical Pharmacology ( 12.3 )]. • Tenofovir disoproxil fumarate increases didanosine concentrations. Dose reduction and close monitoring for didanosine toxicity are warranted.
(7.2) • Coadministration decreases atazanavir concentrations. When coadministered with tenofovir disoproxil fumarate, use atazanavir given with ritonavir. (7.2) • Coadministration of tenofovir disoproxil fumarate with certain HIV-1 protease inhibitors or certain drugs to treat HCV increases tenofovir concentrations.
Monitor for evidence of tenofovir toxicity. (7.2) • Consult Full Prescribing Information prior to and during treatment for important drug interactions. (7.2)
7.1Drugs Affecting Renal Function Tenofovir is primarily eliminated by the kidneys [see Clinical Pharmacology ( 12.3)]. Coadministration of tenofovir disoproxil fumarate tablets with drugs that are eliminated by active tubular secretion may increase concentrations of tenofovir and/or the coadministered drug. Some examples include, but are not limited to, acyclovir, cidofovir, ganciclovir, valacyclovir, valganciclovir, aminoglycosides (e.g., gentamicin), and high-dose or multiple NSAIDs [see Warnings and Precautions ( 5.2)].
Drugs that decrease renal function may increase concentrations of tenofovir. In the treatment of chronic hepatitis B, tenofovir disoproxil fumarate tablets should not be administered in combination with HEPSERA (adefovir dipivoxil).
7.2Established and Significant Interactions Table 11 provides a listing of established or clinically significant drug interactions. The drug interactions described are based on studies conducted with tenofovir DF [see Clinical Pharmacology (12.3)]. Table 11 Established and Significanta Drug Interactions: Alteration in Dose or Regimen May Be Recommended Based on Drug Interaction Trials Concomitant Drug Class: Drug Name Effect on Concentration b Clinical Comment NRTI: didanosine ↑ didanosine Patients receiving tenofovir disoproxil fumarate tablets and didanosine should be monitored closely for didanosine-associated adverse reactions.
Discontinue didanosine in patients who develop didanosine-associated adverse reactions. Higher didanosine concentrations could potentiate didanosine-associated adverse reactions, including pancreatitis, and neuropathy. Suppression of CD4+ cell counts has been observed in patients receiving tenofovir disoproxil fumarate tablets with didanosine 400 mg daily.
In patients weighing greater than 60 kg, reduce the didanosine dose to 250 mg when it is coadministered with tenofovir disoproxil fumarate tablets. In patients weighing less than 60 kg, reduce the didanosine dose to 200 mg when it is coadministered with tenofovir disoproxil fumarate tablets. When coadministered, tenofovir disoproxil fumarate tablets and Videx EC may be taken under fasted conditions or with a light meal (less than 400 kcal, 20% fat).
HIV-1 Protease Inhibitors : atazanavir lopinavir/ritonavir atazanavir/ritonavir darunavir/ritonavir ↓ atazanavir ↑ tenofovir When coadministered with tenofovir disoproxil fumarate tablets, atazanavir 300 mg should be given with ritonavir 100 mg. Monitor patients receiving tenofovir disoproxil fumarate tablets concomitantly with lopinavir/ritonavir, ritonavir-boosted atazanavir, or ritonavir-boosted darunavir for tenofovir DF-associated adverse reactions. Discontinue tenofovir disoproxil fumarate tablets in patients who develop tenofovir DF-associated adverse reactions.
Hepatitis C Antiviral Agents: sofosbuvir/velpatasvir sofosbuvir/velpatasvir/ voxilaprevir ledipasvir/sofosbuvir ↑ tenofovir Monitor patients receiving tenofovir disoproxil fumarate tablets concomitantly with EPCLUSA ® (sofosbuvir/velpatasvir) or VOSEVI ® (sofosbuvir/velpatasvir/voxilaprevir) for adverse reactions associated with tenofovir DF. Monitor patie…
👥 Use in Specific Populations ▾
8 USE IN SPECIFIC POPULATIONS Nursing mothers: Women infected with HIV should be instructed not to breastfeed. (8.3)
8.1Pregnancy Pregnancy Category B There are no adequate and well-controlled studies in pregnant women. Because animal reproduction studies are not always predictive of human response, tenofovir disoproxil fumarate tablets should be used during pregnancy only if clearly needed. Antiretroviral Pregnancy Registry: To monitor fetal outcomes of pregnant women exposed to tenofovir disoproxil fumarate tablets, an Antiretroviral Pregnancy Registry has been established.
Healthcare providers are encouraged to register patients by calling 1-800-258-4263. Risk Summary Animal Data Reproduction studies have been performed in rats and rabbits at doses up to 14 and 19 times the human dose based on body surface area comparisons and revealed no evidence of impaired fertility or harm to the fetus due to tenofovir.
8.3Nursing Mothers Nursing Mothers: The Centers for Disease Control and Prevention recommend that HIV-1 infected mothers not breastfeed their infants to avoid risking postnatal transmission of HIV-1. Samples of breast milk obtained from five HIV-1 infected mothers in the first post-partum week show that tenofovir is secreted in human milk. The impact of this exposure in breastfed infants is unknown.
Because of both the potential for HIV-1 transmission and the potential for serious adverse reactions in nursing infants, mothers should be instructed not to breastfeed if they are receiving tenofovir disoproxil fumarate tablets.
8.4Pediatric Use Pediatric Patients 2 Years of Age and Older with HIV-1 infection The safety of tenofovir disoproxil fumarate tablets in pediatric patients aged 2 to less than 18 years is supported by data from two randomized trials in which tenofovir disoproxil fumarate tablets were administered to HIV-1 infected treatment-experienced subjects. In addition, the pharmacokinetic profile of tenofovir in patients 2 to less than 18 years of age at the recommended doses was similar to that found to be safe and effective in adult clinical trials [See Clinical Pharmacology ( 12.3)].
In Study 352, 92 treatment-experienced subjects 2 to less than 12 years of age with stable, virologic suppression on stavudine- or zidovudine-containing regimen were randomized to either replace stavudine or zidovudine with tenofovir disoproxil fumarate tablets (N=44) or continue their original regimen (N=48) for 48 weeks. Five additional subjects over the age of 12 were enrolled and randomized (tenofovir disoproxil fumarate tablets N=4, original regimen N=1) but are not included in the efficacy analysis. After 48 weeks, all eligible subjects were allowed to continue in the study receiving open-label tenofovir disoproxil fumarate tablets.
At Week 48, 89% of subjects in the tenofovir disoproxil fumarate treatment group and 90% of subjects in the stavudine or zidovudine treatment group had HIV-1 RNA concentrations less than 400 copies/mL. During the 48 week randomized phase of the study, 1 subject in the tenofovir disoproxil fumarate tablets group discontinued the study prematurely because of virologic failure/lack of efficacy and 3 subjects (2 subjects in the tenofovir disoproxil fumarate tablets group and 1 subject in the stavudine or zidovudine group) discontinued for other reasons.
In Study 321, 87 treatment-experienced subjects 12 to less than 18 years of age were treated with tenofovir disoproxil fumarate tablets (N=45) or placebo (N=42) in combination with an optimized background regimen (OBR) for 48 weeks. The mean baseline CD4 cell count was 374 cells/mm 3 and the mean baseline plasma HIV-1 RNA was 4.6 log 10 copies/mL. At baseline, 90% of subjects harbored NRTI resistance-associated substitutions in their HIV-1 isolates.
Overall, the trial failed to show a difference in virologic response between the tenofovir disoproxil fumarate tablets and placebo treatment groups. Subgroup analyses suggest the lack of difference in…
🤰 Pregnancy ▾
8.1Pregnancy Pregnancy Category B There are no adequate and well-controlled studies in pregnant women. Because animal reproduction studies are not always predictive of human response, tenofovir disoproxil fumarate tablets should be used during pregnancy only if clearly needed. Antiretroviral Pregnancy Registry: To monitor fetal outcomes of pregnant women exposed to tenofovir disoproxil fumarate tablets, an Antiretroviral Pregnancy Registry has been established.
Healthcare providers are encouraged to register patients by calling 1-800-258-4263. Risk Summary Animal Data Reproduction studies have been performed in rats and rabbits at doses up to 14 and 19 times the human dose based on body surface area comparisons and revealed no evidence of impaired fertility or harm to the fetus due to tenofovir.
🧒 Pediatric Use ▾
8.4Pediatric Use Pediatric Patients 2 Years of Age and Older with HIV-1 infection The safety of tenofovir disoproxil fumarate tablets in pediatric patients aged 2 to less than 18 years is supported by data from two randomized trials in which tenofovir disoproxil fumarate tablets were administered to HIV-1 infected treatment-experienced subjects. In addition, the pharmacokinetic profile of tenofovir in patients 2 to less than 18 years of age at the recommended doses was similar to that found to be safe and effective in adult clinical trials [See Clinical Pharmacology ( 12.3)].
In Study 352, 92 treatment-experienced subjects 2 to less than 12 years of age with stable, virologic suppression on stavudine- or zidovudine-containing regimen were randomized to either replace stavudine or zidovudine with tenofovir disoproxil fumarate tablets (N=44) or continue their original regimen (N=48) for 48 weeks. Five additional subjects over the age of 12 were enrolled and randomized (tenofovir disoproxil fumarate tablets N=4, original regimen N=1) but are not included in the efficacy analysis. After 48 weeks, all eligible subjects were allowed to continue in the study receiving open-label tenofovir disoproxil fumarate tablets.
At Week 48, 89% of subjects in the tenofovir disoproxil fumarate treatment group and 90% of subjects in the stavudine or zidovudine treatment group had HIV-1 RNA concentrations less than 400 copies/mL. During the 48 week randomized phase of the study, 1 subject in the tenofovir disoproxil fumarate tablets group discontinued the study prematurely because of virologic failure/lack of efficacy and 3 subjects (2 subjects in the tenofovir disoproxil fumarate tablets group and 1 subject in the stavudine or zidovudine group) discontinued for other reasons.
In Study 321, 87 treatment-experienced subjects 12 to less than 18 years of age were treated with tenofovir disoproxil fumarate tablets (N=45) or placebo (N=42) in combination with an optimized background regimen (OBR) for 48 weeks. The mean baseline CD4 cell count was 374 cells/mm 3 and the mean baseline plasma HIV-1 RNA was 4.6 log 10 copies/mL. At baseline, 90% of subjects harbored NRTI resistance-associated substitutions in their HIV-1 isolates.
Overall, the trial failed to show a difference in virologic response between the tenofovir disoproxil fumarate tablets and placebo treatment groups. Subgroup analyses suggest the lack of difference in virologic response may be attributable to imbalances between treatment arms in baseline viral susceptibility to tenofovir disoproxil fumarate tablets and OBR. Although changes in HIV-1 RNA in these highly treatment-experienced subjects were less than anticipated, the comparability of the pharmacokinetic and safety data to that observed in adults supports the use of tenofovir disoproxil fumarate tablets in pediatric patients 12 years of age and older who weigh greater than or equal to 35 kg and whose HIV-1 isolate is expected to be sensitive to tenofovir disoproxil fumarate tablets. [See Warnings and Precautions (5.6), Adverse Reactions (6.1), and Clinical Pharmacology ( 12.3)].
Safety and effectiveness of tenofovir disoproxil fumarate tablets in pediatric patients younger than 2 years of age with HIV-1 infection have not been established. Pediatric Patients 12 Years of Age and Older with Chronic Hepatitis B In Study 115, 106 HBeAg negative (9%) and positive (91%) subjects aged 12 to less than 18 years with chronic HBV infection were randomized to receive blinded treatment with tenofovir disoproxil fumarate tablets 300 mg (N=52) or placebo (N=54) for 72 weeks. At study entry, the mean HBV DNA was 8.1 log10 copies/mL and mean ALT was 101 U/L.
Of 52 subjects treated with tenofovir disoproxil fumarate tablets, 20 subjects were nucleos(t)ide-naïve and 32 subjects were nucleos(t)ide-experienced. Thirty-one of the 32 nucleos(t)ide-experienced subjects had prior lamivudine experience. At Week 72, 88% (46/52) of subjects in the tenofovir dis…
🧓 Geriatric Use ▾
8.5Geriatric Use Clinical trials of tenofovir disoproxil fumarate tablets did not include sufficient numbers of subjects aged 65 and over to determine whether they respond differently from younger subjects. In general, dose selection for the elderly patient should be cautious, keeping in mind the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy.
🆘 Overdosage ▾
10 OVERDOSAGE Limited clinical experience at doses higher than the therapeutic dose of tenofovir disoproxil fumarate tablets 300 mg are available. In Study 901, 600 mg tenofovir DF was administered to 8 subjects orally for 28 days. No severe adverse reactions were reported.
The effects of higher doses are not known. If overdose occurs the patient must be monitored for evidence of toxicity and standard supportive treatment applied as necessary. Tenofovir is efficiently removed by hemodialysis with an extraction coefficient of approximately 54%.
Following a single 300 mg dose of tenofovir disoproxil fumarate tablets, a four-hour hemodialysis session removed approximately 10% of the administered tenofovir dose.
🧬 Clinical Pharmacology ▾
12 CLINICAL PHARMACOLOGY
12.1Mechanism of Action Tenofovir disoproxil fumarate is an antiviral drug [See Microbiology ( 12.4 )].
12.3Pharmacokinetics The pharmacokinetics of tenofovir DF have been evaluated in healthy volunteers and HIV-1 infected individuals. Tenofovir pharmacokinetics are similar between these populations. Absorption Tenofovir disoproxil fumarate tablets are a water soluble diester prodrug of the active ingredient tenofovir.
The oral bioavailability of tenofovir from tenofovir disoproxil fumarate tablets in fasted subjects is approximately 25%. Following oral administration of a single dose of tenofovir disoproxil fumarate tablets 300 mg to HIV-1 infected subjects in the fasted state, maximum serum concentrations (C max ) are achieved in 1 ± 0.4 hrs. C max and AUC values are 0.30 ± 0.09 mcg/mL and 2.29 ± 0.69 mcg·hr/mL, respectively.
The pharmacokinetics of tenofovir are dose proportional over a tenofovir disoproxil fumarate tablets dose range of 75 to 600 mg and are not affected by repeated dosing. Distribution In vitro binding of tenofovir to human plasma or serum proteins is less than 0.7 and 7.2%, respectively, over the tenofovir concentration range 0.01 to 25 mcg/mL. The volume of distribution at steady-state is 1.3 ±
0.6L/kg and 1.2 ±
0.4L/kg, following intravenous administration of tenofovir 1 mg/kg and 3 mg/kg. Metabolism and Elimination In vitro studies indicate that neither tenofovir disoproxil nor tenofovir are substrates of CYP enzymes. Following IV administration of tenofovir, approximately 70 to 80% of the dose is recovered in the urine as unchanged tenofovir within 72 hours of dosing.
Following single dose, oral administration of tenofovir disoproxil fumarate tablets, the terminal elimination half-life of tenofovir is approximately 17 hours. After multiple oral doses of tenofovir disoproxil fumarate tablets 300 mg once daily (under fed conditions), 32 ± 10% of the administered dose is recovered in urine over 24 hours. Tenofovir is eliminated by a combination of glomerular filtration and active tubular secretion.
There may be competition for elimination with other compounds that are also renally eliminated. Effects of Food on Oral Absorption Administration of tenofovir disoproxil fumarate 300 mg tablets following a high-fat meal (~700 to 1,000 kcal containing 40 to 50% fat) increases the oral bioavailability, with an increase in tenofovir AUC 0 to ∞ of approximately 40% and an increase in C max of approximately 14%. However, administration of tenofovir disoproxil fumarate tablets with a light meal did not have a significant effect on the pharmacokinetics of tenofovir when compared to fasted administration of the drug.
Food delays the time to tenofovir C max by approximately 1 hour. C max and AUC of tenofovir are 0.33 ± 0.12 mcg/mL and 3.32 ± 1.37 mcg·hr/mL following multiple doses of tenofovir disoproxil fumarate tablets 300 mg once daily in the fed state, when meal content was not controlled. Special Populations Race: There were insufficient numbers from racial and ethnic groups other than Caucasian to adequately determine potential pharmacokinetic differences among these populations.
Gender: Tenofovir pharmacokinetics are similar in male and female subjects. Pediatric Patients 2 Years of Age and Older: Steady-state pharmacokinetics of tenofovir were evaluated in 31 HIV-1 infected pediatric subjects 2 to less than 18 years (Table 12). Tenofovir exposure achieved in these pediatric subjects receiving oral once daily doses of tenofovir disoproxil fumarate tablets 300 mg up to a maximum dose of 300 mg was similar to exposures achieved in adults receiving once-daily doses of tenofovir disoproxil fumarate tablets 300 mg.
Table 12 Mean (± SD) Tenofovir Pharmacokinetic Parameters by Age Groups for HIV-1- infected Pediatric Patients Dose and Formulation 300 mg tablet 12 to <18 Years (N=8) C max (mcg/mL) 0.38 ±
0.13AUC tau (mcg•hr/mL) 3.39 ±
1.22 Tenofovir exposures in 52 HBV-infected pediatric su…
🧬 Mechanism of Action ▾
12.1Mechanism of Action Tenofovir disoproxil fumarate is an antiviral drug [See Microbiology ( 12.4 )].
📦 How Supplied / Storage and Handling ▾
16 HOW SUPPLIED/STORAGE AND HANDLING Tablets Tenofovir disoproxil fumarate tablets, 300 mg, are white colored, almond shaped, film coated tablets contain 300 mg of tenofovir DF, which is equivalent to 245 mg of tenofovir disoproxil, are debossed with .H. on one side and .123. on other side. They are packaged as follows: Bottle of 30 tablets (NDC 16714-820-01) Store at 20° to 25°C (68° to 77°F) [see USP Controlled Room Temperature]. Keep the bottle tightly closed.
Do not use if seal over bottle opening is broken or missing.
📋 Description ▾
11 DESCRIPTION Tenofovir disoproxil fumarate tablet a prodrug of tenofovir which is a fumaric acid salt of bis-isopropoxycarbonyloxymethyl ester derivative of tenofovir. In vivo tenofovir DF is converted to tenofovir, an acyclic nucleoside phosphonate (nucleotide) analog of adenosine 5’-monophosphate. Tenofovir exhibits activity against HIV-1 reverse transcriptase.
The chemical name of tenofovir DF is 9-[(R)-2-[[bis[[(isopropoxycarbonyl)oxy]methoxy]phosphinyl]methoxy]propyl] adenine fumarate (1:1). It has a molecular formula of C 19 H 30 N 5 O 10 P • C 4 H 4 O 4 and a molecular weight of 635.52. It has the following structural formula: Tenofovir DF is a white to off-white crystalline powder with a solubility of 13.4 mg/mL in distilled water at 25°C.
It has an octanol/phosphate buffer (pH 6.5) partition coefficient (log p) of 1.25 at 25 °C. Tenofovir disoproxil fumarate is available as tablets. Tenofovir disoproxil fumarate tablets are for oral administration.
Each tablet contains 300 mg of tenofovir DF, which is equivalent to 245 mg of tenofovir disoproxil. Each tablet contains the following inactive ingredients: croscarmellose sodium, lactose monohydrate, magnesium stearate, microcrystalline cellulose and pregelatinized starch. The 300 mg tablets are coated with opadry II white which contains hypromellose, lactose monohydrate, titanium dioxide and triacetin.
In this insert, all dosages are expressed in terms of tenofovir DF except where otherwise noted. Tenofovirdisoproxilfumaratestructure
💬 Information for Patients ▾
17 PATIENT COUNSELING INFORMATION Advise the patient to read the FDA-approved patient labeling (Patient Information). Inform patients that tenofovir disoproxil fumarate tablets are not a cure for HIV-1 infection and patients may continue to experience illnesses associated with HIV-1 infection, including opportunistic infections. Patients should remain under the care of a physician when using tenofovir disoproxil fumarate tablets.
Advise patients to avoid doing things that can spread HIV or HBV to others. • Do not share needles or other injection equipment. • Do not share personal items that can have blood or body fluids on them, like toothbrushes and razor blades. • Do not have any kind of sex without protection. Always practice safer sex by using a latex or polyurethane condom to lower the chance of sexual contact with semen, vaginal secretions, or blood. • Do not breastfeed. Tenofovir is excreted in breast milk and it is not known whether it can harm the baby.
Mothers with HIV-1 should not breastfeed because HIV-1 can be passed to the baby in the breast milk. Inform patients that: • The long-term effects of tenofovir disoproxil fumarate tablets are unknown. • Tenofovir disoproxil fumarate tablets are for oral ingestion only. • Tenofovir disoproxil fumarate tablets should not be discontinued without first informing their physician. • If you have HIV-1 infection, with or without HBV coinfection, it is important to take tenofovir disoproxil fumarate tablets with combination therapy. • It is important to take tenofovir disoproxil fumarate tablets on a regular dosing schedule and to avoid missing doses. • Severe acute exacerbations of hepatitis have been reported in patients who are infected with HBV or coinfected with HBV and HIV-1 and have discontinued tenofovir disoproxil fumarate tablets [See Warnings and Precautions (5.1)]. • Renal impairment, including cases of acute renal failure and Fanconi syndrome, has been reported.
Tenofovir disoproxil fumarate tablets should be avoided with concurrent or recent use of a nephrotoxic agent (e.g., high-dose or multiple NSAIDs) [See Warnings and Precautions (5.2)]. • Lactic acidosis and severe hepatomegaly with steatosis, including fatal cases, have been reported. Treatment with tenofovir disoproxil fumarate tablets should be suspended in any patient who develops clinical symptoms suggestive of lactic acidosis or pronounced hepatotoxicity [See Warnings and Precautions (5.3)]. • Tenofovir disoproxil fumarate tablets should not be coadministered with ATRIPLA, BIKTARVY, COMPLERA, DESCOVY, GENVOYA, ODEFSEY, STRIBILD, TRUVADA, or VEMLIDY [See Warnings and Precautions ( 5.4)]. • Tenofovir disoproxil fumarate tablets should not be administered in combination with HEPSERA [See Warnings and Precautions (5.4)]. • Decreases in bone mineral density have been observed with the use of tenofovir disoproxil fumarate tablets.
Bone mineral density monitoring should be considered in patients who have a history of pathologic bone fracture or at risk for osteopenia [See Warnings and Precautions ( 5.6)]. • In some patients treated with combination antiretroviral therapy, including tenofovir disoproxil fumarate tablets, signs and symptoms of inflammation from previous infections may occur soon after anti-HIV treatment is started. It is believed that these symptoms are due to an improvement in the body’s immune response, enabling the body to fight infections that may have been present with no obvious symptoms.
Advise patients to inform their healthcare provider immediately of any symptoms of infection [See Warnings and Precautions (5.7)]. • In the treatment of chronic hepatitis B, the optimal duration of treatment is unknown. The relationship between response and long-term prevention of outcomes such as hepatocellular carcinoma is not known. All brand names listed are the registered trademarks of their respective owners and are not trademarks of Hetero Labs Limited.
Manufactured for: Northstar Rx LLC Memphis, T…