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.
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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 3SY5LH9PMK
Anhydrous lactose is a milk sugar with no water content. It acts as a filler and binder in tablets and capsules, adding bulk and helping ingredients stick together.
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UNII 776XM7047L
Calcium stearate is a white powder derived from stearic acid and calcium. It works as a lubricant and glidant to help the medicine flow smoothly during manufacturing and prevent ingredients from sticking to equipment.
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UNII 2S7830E561
Crospovidone is a synthetic polymer derived from povidone. It acts as a disintegrant, helping the tablet or capsule break apart quickly in the stomach so the active ingredient can be absorbed.
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A synthetic blue dye approved by the FDA for use in medications and foods. It serves as a colorant to make pills and liquids visually distinct and easier to identify.
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UNII Q662QK8M3B
Polyethylene glycol 8000 is a synthetic polymer made from ethylene oxide. It acts as a binder and filler in tablets and capsules, helping hold ingredients together and add bulk to the medicine.
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UNII 532B59J990
Polyvinyl alcohol is a synthetic polymer made from plant-derived materials. It's used as a binder to hold ingredients together, a film-former in coatings, and a thickener in liquid formulations.
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UNII ETJ7Z6XBU4
Silicon dioxide is a naturally occurring mineral used as a glidant and anti-caking agent. It helps powder ingredients flow smoothly and prevents clumping during manufacturing and storage.
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A powder made from a naturally occurring mineral. In medicines, talc works as a glidant and anti-caking agent, helping tablets and capsules flow smoothly during manufacturing and preventing clumping.
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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.
9 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 | $0.294 | $8.81 / 30 tablets |
| Medicaid paysCMS SDUD · 12 mo | No recent Medicaid claims on file for this NDC — rare and low-volume NDCs are suppressed in the public data. | |
| Medicare drug plans payPart D · Q2 2026 | $1.04 | $31.29 / 30 tablets |
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🔁 Therapeutic equivalents
| Product | Labeler | Pack | NADAC/unit | TE | Status | Price vs. this |
|---|---|---|---|---|---|---|
| tenofovir disoproxil fumarate 300 mg 00904-6821-04 | Major | 30 tablets | $0.294 | AB | Availability likely | — |
| Tenofovir Disoproxil Fumarate 300 mg 16714-0820-01 | NorthStar | 30 tablets | $0.294 | AB | Availability likely | — |
| tenofovir disoproxil fumarate 300 mg 33342-0096-07 | Macleods | 30 tablets | $0.294 | AB | Availability likely | — |
| Tenofovir Disoproxil Fumarate 300 mg 50268-0758-12 | AvPAK | 20 tablets | $0.294 | AB | Availability likely | — |
| Tenofovir Disoproxil Fumarate 300 mgthis 62135-0466-30 | Chartwell | 30 tablets | $0.294 | AB | Availability likely | — |
| Tenofovir Disoproxil Fumarate 300 mg 64380-0714-04 | Strides | 30 tablets | $0.294 | AB | Availability likely | — |
| Tenofovir Disoproxil Fumarate 300 mg 65862-0421-30 | Aurobindo | 30 tablets | $0.294 | — | Availability likely | — |
| Tenofovir Disoproxil Fumarate 300 mg 69076-0105-03 | Quinn | 30 tablets | $0.294 | AB | Availability likely | — |
| Tenofovir disoproxil fumarate 300 mg 69097-0533-02 | Cipla | 30 tablets | $0.294 | AB | Availability likely | — |
| Tenofovir Disoproxil Fumarate 300 mg 71921-0105-33 | Florida | 30 tablets | $0.294 | AB | Availability likely | — |
| Viread 300 mg 61958-0401-01 | Gilead | 30 tablets | $40.687 | AB | Availability likely | +13748% |
| 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 | — |
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?
📊 Medicare Part D spend CMS · PART D · 2026 (Q1)
📦 Packaging — all sizes for this product
| Package NDC | Description | Marketing start | Status |
|---|---|---|---|
| 62135-0466-30 You're viewing this | 30 TABLET, FILM COATED in 1 BOTTLE (62135-466-30) | 2022-06-30 | Active |
📄 Full prescribing information FDA SPL
🚨 Boxed Warning ▾
WARNING: POSTTREATMENT ACUTE EXACERBATION OF HEPATITIS B Severe acute exacerbations of hepatitis B virus (HBV) have been reported in HBV-infected patients who have discontinued anti-hepatitis B therapy, including tenofovir disoproxil fumarate. Hepatic function should be monitored closely with both clinical and laboratory follow-up for at least several months in HBV-infected patients who discontinue anti-hepatitis B therapy, including tenofovir disoproxil fumarate. If appropriate, resumption of anti-hepatitis B therapy may be warranted [see Warnings and Precautions ( 5.1 )] .
WARNING: POSTTREATMENT ACUTE EXACERBATION OF HEPATITIS B S e e full prescribing information for complete boxed warning. Severe acute exacerbations of hepatitis B virus (HBV) have been reported in HBV-infected patients who have discontinued anti-hepatitis B therapy, including tenofovir disoproxil fumarate. Hepatic function should be monitored closely in HBV-infected patients who discontinue tenofovir disoproxil fumarate.
If appropriate, resumption of anti-hepatitis B therapy may be warranted. ( 5.1 )
🎯 Indications and Usage ▾
1 INDICATIONS AND USAGE Tenofovir disoproxil fumarate tablets are a nucleotide analog HIV-1 reverse transcriptase inhibitor and an HBV reverse transcriptase inhibitor and is 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 weighing at least 10 kg. ( 1.1 ) for the treatment of chronic hepatitis B in adults and pediatric patients 2 years and older weighing at least 10 kg. ( 1.2 )
1.1HIV-1 Infection Tenofovir disoproxil fumarate tablets are indicated in combination with other antiretroviral agents for the treatment of human immunodeficiency virus type 1 (HIV-1) infection in adults and pediatric patients 2 years of age and older weighing at least 10 kg.
1.2Chronic Hepatitis B Tenofovir disoproxil fumarate tablets are indicated for the treatment of chronic hepatitis B virus (HBV) in adults and pediatric patients 2 years of age and older weighing at least 10 kg.
⏱️ Dosage and Administration ▾
2 DOSAGE AND ADMINISTRATION Testing: Prior to or when initiating tenofovir disoproxil fumarate tablets test for hepatitis B virus infection and HIV-1 infection. Prior to initiation and during use of Tenofovir disoproxil fumarate tablets, on a clinically appropriate schedule, assess serum creatinine, estimated creatinine clearance, urine glucose, and urine protein in all patients. In patients with chronic kidney disease, also assess serum phosphorous.
( 2.1 ) Recommended tablet dosage in adults and pediatric patients weighing at least 35 kg: One tenofovir disoproxil fumarate 300 mg tablet once daily taken orally without regard to food. ( 2.2 ) Recommended dosage in pediatric patients at least 2 years of age and adults: Tablets: For patients weighing at least 17 kg who can swallow an intact tablet, one tenofovir disoproxil fumarate tablet (150 mg, 200 mg, 250 mg, or 300 mg based on body weight) once daily taken orally without regard to food. ( 2.2 ) Recommended dosage in renally impaired adult patients: Creatinine clearance (CrCL) 30 to 49 mL/min: 300 mg every 48 hours.
( 2.4 ) CrCL10 to 29 mL/min: 300 mg every 72 to 96 hours. ( 2.4 ) Hemodialysis: 300 mg every 7 days or after approximately 12 hours of dialysis. ( 2.4 )
2.1Testing Prior to Initiation of tenofovir disoproxil fumarate tablets for Treatment of HIV-1 Infection or Chronic Hepatitis B Prior to or when initiating tenofovir disoproxil fumarate tablets, test patients for HBV infection and HIV-1 infection. Tenofovir disoproxil fumarate tablets alone should not be used in patients with HIV-1 infection [see Warnings and Precautions ( 5.3 )]. Prior to initiation and during use of tenofovir disoproxil fumarate tablets, on a clinically appropriate schedule, assess serum creatinine, estimated creatinine clearance, urine glucose and urine protein in all patients.
In patients with chronic kidney disease, also assess serum phosphorus [see Warnings and Precautions ( 5.2 )].
2.2Recommended Tablet Dosage in Adults and Pediatric Patients 2 Years and Older Weighing at Least 17 kg The recommended dosage of tenofovir disoproxil fumarate tablet in adults and pediatric patients weighing at least 35 kg is one 300 mg tablet taken orally once daily without regard to food. The dosage for tenofovir disoproxil fumarate tablets is the same for both HIV and HBV indications. The recommended dosage of tenofovir disoproxil fumarate tablets tablet in adults and pediatric patients 2 years and older weighing at least 17 kg is 8 mg of tenofovir disoproxil fumarate (TDF) per kg of body weight (up to a maximum of 300 mg) once daily.
Dosage for pediatric patients 2 years and older weighing between 17 kg and 35 kg and able to swallow an intact tablet is provided in Table 1. Weight should be monitored periodically and the tenofovir disoproxil fumarate tablets dose adjusted accordingly. Table 1 Recommended Dosing for Patients 2 Years and Older and Weighing at Least 17 kg Using Tenofovir Disoproxil Fumarate Tablets Body Weight (kg) Dosing of Tenofovir Disoproxil Fumarate T ablets 17 to less than 22 one 150 mg tablet once daily 22 to less than 28 one 200 mg tablet once daily 28 to less than 35 one 250 mg tablet once daily at least 35 one 300 mg tablet once daily
2.4Dosage Adjustment in Patients with Renal Impairment Significant increase in drug exposures occurred when tenofovir disoproxil fumarate tablets were administered to subjects with moderate to severe renal impairment (creatinine clearance below 50 mL/min). Table 3 provides dosage interval adjustment for patients with renal impairment. No dosage adjustment of tenofovir disoproxil fumarate tablets 300 mg is necessary for patients with mild renal impairment (creatinine clearance 50 to 80 mL/min) [see Warnings and Precautions ( 5.3 ), Use in Specific Populations ( 8.6 ), and Clinical Pharmacology ( 12.3 ) ] .
Table 3 Dosage Interval Adjustment for Adult Patients with Altered Creatinine Clearance Creatinine Clearance (mL/min) a Hemodialysis Patients 50 or…
💊 Dosage Forms and Strengths ▾
3 DOSAGE FORMS AND STRENGTHS Tenofovir disoproxil fumarate tablets 300 mg contain 300 mg of tenofovir disoproxil fumarate, which is equivalent to 245 mg of tenofovir disoproxil. The tablets are light blue, oval shaped, film-coated tablets, debossed “CE 54” on one side, and plain on the other side. Tablets: 300 mg of tenofovir disoproxil fumarate. ( 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. Avoid administering tenofovir disoproxil fumarate with concurrent or recent use of nephrotoxic drugs. ( 5.2 ) HIV testing: HIV antibody testing should be offered to all HBV-infected patients before initiating therapy with tenofovir disoproxil fumarate.
Tenofovir disoproxil fumarate should only be used as part of an appropriate antiretroviral combination regimen in HIV-infected patients with or without HBV coinfection. ( 5.3 ) Immune reconstitution syndrome: May necessitate further evaluation and treatment. ( 5.4 ) 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.
( 5.5 ) Lactic acidosis/severe hepatomegaly with steatosis: Discontinue treatment in patients who develop symptoms or laboratory findings suggestive of lactic acidosis or pronounced hepatotoxicity. ( 5.6 )
5.1Severe Acute Exacerbation of Hepatitis B in Patients with HBV Infection All patients should be tested for the presence of chronic hepatitis B virus (HBV) before or when initiating tenofovir disoproxil fumarate [see Dosage and Administration ( 2.1 )] . Discontinuation of anti-HBV therapy, including tenofovir disoproxil fumarate, may be associated with severe acute exacerbations of hepatitis B. Patients infected with HBV who discontinue tenofovir disoproxil fumarate 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, especially in patients with advanced liver disease or cirrhosis, since posttreatment exacerbation of hepatitis may lead to hepatic decompensation and liver failure.
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 [see Adverse Reactions ( 6.2 )] . Prior to initiation and during use of tenofovir disoproxil fumarate, on a clinically appropriate schedule, assess serum creatinine, estimated creatinine clearance, urine glucose, and urine protein in all patients.
In patients with chronic kidney disease, also assess serum phosphorus. 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 ( 2.4 )] . No safety or efficacy data are available in patients with renal impairment who received tenofovir disoproxil fumarate using these dosing guidelines, so the potential benefit of tenofovir disoproxil fumarate 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 after initiation of high-dose or multiple NSAIDs have been reported in HIV-infected patients with risk factors for renal dysfunction who appeared stable on TDF. Some patients required hospitalization and renal replacement therapy.
Alternatives to NSAIDs should be considered, if needed, in patients at risk for renal dysfunction. Persistent or worsening bone pain, pain in extremities, fractures and/or muscular pain or weakness may be manifestations of proximal renal tubulopathy and should prompt an evaluation of renal function in patients at risk of renal dysfunction.
5.3Patients Coinfected with HIV-1 and HBV Due to the risk of development of HIV-1 resistance, tenofovir disoproxil fumarate should only be used in HIV-1 and HBV coinfected patients as part of an appropriate a…
🤒 Adverse Reactions ▾
6 ADVERSE REACTIONS The following adverse reactions are discussed in other sections of the labeling: Severe Acute Exacerbation of Hepatitis B in Patients with HBV Infection [see Warnings and Precautions ( 5.1 )] . New Onset or Worsening Renal Impairment [see Warnings and Precautions ( 5.2 )] . Immune Reconstitution Syndrome [see Warnings and Precautions ( 5.4 )] .
Bone Loss and Mineralization Defects [see Warnings and Precautions ( 5.5 )] . Lactic Acidosis/Severe Hepatomegaly with Steatosis [see Warnings and Precautions ( 5.6 )] . In HIV-infected adult subjects: Most common adverse reactions (incidence greater than or equal to 10%, Grades 2 to 4) were rash, diarrhea, nausea, headache, pain, depression, and asthenia.
( 6.1 ) In HBV-infected subjects with compensated liver disease: Most common adverse reaction (all grades) was nausea (9%). ( 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 ) In pediatric subjects: Adverse reactions in pediatric subjects were consistent with those observed in adults.
( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Chartwell RX, LLC. at 1-845-232-1683 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch .
6.1Clinical 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. Adverse Reactions from Clinical Trials Experience in HIV-1 Infected Adults More than 12,000 subjects have been treated with tenofovir disoproxil fumarate 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 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. Clinical Trials in Treatment-Naïve HIV-1 Infected Adult Subjects In Trial 903, 600 antiretroviral- naïve subjects received tenofovir disoproxil fumarate (N=299) or stavudine (d4T) (N=301) administered in combination with lamivudine (3TC) and efavirenz (EFV) for 144 weeks.
The most common adverse reactions 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. Table 4 provides the treatment-emergent adverse reactions (Grades 2−4) occurring in greater than or equal to 5% of subjects treated in any treatment group.
Table 4 Selected Adverse Reactions a (Grades 2 to 4) Reported in ≥5% in Any Treatment Group in Trial 903 (0 to 144 Weeks) Tenofovir disoproxil fumarate + 3 T C+EFV d4T+3TC+EFV N=299 N=301 Rash event b 18% 12% Headache 14% 17% Pain 13% 12% Diarrhea 11% 13% Depression 11% 10% Back pain 9% 8% Nausea 8% 9% Fever 8% 7% Abdominal pain 7% 12% Asthenia 6% 7% Anxiety 6% 6% Vomiting 5% 9% Insomnia 5% 8% Arthralgia 5% 7% Pneumonia 5% 5% Dyspepsia 4% 5% Dizziness 3% 6% Myalgia 3% 5% Lipodystrophyc 1% 8% Peripheral neuropathy d 1% 5% a.
Frequencies of adverse reactions are based on all treatment-emergent adverse events, regardless of relationship to study drug. b. Rash event includes rash, pruritus, maculopapular rash, urticaria, vesiculobullous rash, and pustular rash. c. Lipodystrophy represents a variety of investigator-described adverse events not a protocol-defined syndrome. d.
Peripheral neuropathy includes peripheral neuritis and neuropathy. La b o r a tor…
🔄 Drug Interactions ▾
7 DRUG INTERACTIONS 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 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 should not be administered in combination with HEPSERA (adefovir dipivoxil).
7.2Established and Significant Interactions Table 12 provides a listing of established or clinically significant drug interactions. The drug interactions described are based on studies conducted with TDF [see Clinical Pharmacology ( 12.3 )]. T ab l e 12 Established and Significant a D rug 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 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. In patients weighing less than 60 kg, reduce the didanosine dose to 200 mg when it is coadministered with tenofovir disoproxil fumarate. When coadministered, tenofovir disoproxil fumarate 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 ↓ atazanavir When coadministered with tenofovir disoproxil fumarate tablets, atazanavir 300 mg should be given with ritonavir 100 mg. lopinavir/ritonavir atazanavir/ritonavir darunavir/ritonavir ↑ tenofovir Monitor patients receiving tenofovir disoproxil fumarate tablets concomitantly with lopinavir/ritonavir, ritonavir-boosted atazanavir, or ritonavir-boosted darunavir for TDF-associated adverse reactions. Discontinue tenofovir disoproxil fumarate tablets in patients who develop TDF-associated adverse reactions.
Hepatitis C Antiviral Agents: sofosbuvir/velpatasvir sofosbuvir/velpatasvir/voxilaprevir ↑ tenofovir Monitor patients receiving tenofovir disoproxil fumarate tablets concomitantly with EPCLUSA ® (sofosbuvir/velpatasvir) for adverse reactions associated with TDF. ledipasvir/sofosbuvir Monitor patients receiving tenofovir disoproxil fumarate tablets concomitantly with HARVONI ® (ledipasvir/sofosbuvir) without an HIV-1 protease inhibitor/ritonavir or an HIV-1 protease inhibitor/cobicistat combination for adverse reactions associated with TDF.
In patients receiving tenofovir disoproxil fumarate tablets concomitantly with HARV…
👥 Use in Specific Populations ▾
8 USE IN SPECIFIC POPULATIONS Lactation: Breastfeeding in HIV-1 : infected mothers is not recommended due to the potential for HIV-1 transmission. ( 8.2 )
8.1Pregnancy P r eg n an cy Exposure Registry There is a pregnancy exposure registry that monitors pregnancy outcomes in women exposed to tenofovir disoproxil fumarate during pregnancy. Healthcare providers are encouraged to register patients by calling the Antiretroviral Pregnancy Registry (APR) at 1-800-258-4263. Risk Summary Available data from the APR show no increase in the overall risk of major birth defects with first trimester exposure for tenofovir disoproxil fumarate (TDF) (2.1%) compared with the background rate for major birth defects of 2.7% in a U.S. reference population of the Metropolitan Atlanta Congenital Defects Program (MACDP) (see Data).
The rate of miscarriage for individual drugs is not reported in the APR. In the U.S. general population, the estimated background risk of miscarriage in clinically recognized pregnancies is 15–20%. Published studies in HBV-infected subjects do not report an increased risk of adverse pregnancy- related outcomes with the use of tenofovir disoproxil fumarate during the third trimester of pregnancy (see Data).
In animal reproduction studies, no adverse developmental effects were observed when TDF was administered at doses/exposures ≥14 (TDF) and 2.7 (tenofovir) times those of the recommended daily dose of tenofovir disoproxil fumarate tablets (see Data). Data Human Data Based on prospective reports from the APR exposures to TDF-containing regimens during pregnancy resulting in live births (including 3,342 exposed in the first trimester and 1,475 exposed in the second/third trimester), there was no increase in overall major birth defects with TDF compared with the background birth defect rate of 2.7% in a U.S. reference population of the MACDP.
The prevalence of major birth defects in live births was 2.3% (95% CI: 1.8% to 2.8%) with first trimester exposure to TDF-containing regimens, and 2.1% (95% CI: 1.4% to 3.0%) with the second/third trimester exposure to TDF-containing regimens. Prospective reports from the APR of overall major birth defects in pregnancies exposed to TDF are compared with a U.S. background major birth defect rate. Methodological limitations of the APR include the use of MACDP as the external comparator group.
Limitations of using an external comparator include differences in methodology and populations, as well as confounding due to the underlying disease. In published data from three controlled clinical trials, a total of 327 pregnant women with chronic HBV infection were administered tenofovir disoproxil fumarate from 28 to 32 weeks gestation through 1 to 2 months postpartum and followed for up to 12 months after delivery. There were no new safety findings in pregnant women compared with the known safety profile of tenofovir disoproxil fumarate in HBV-infected adults.
An increased risk of adverse pregnancy-related outcomes was not observed; 2 stillbirths were identified, and there was 1 major birth defect (talipes) and 1 occurrence of multiple congenital abnormalities (not further specified) in tenofovir disoproxil fumarate -exposed infants. Infants were followed for up to 12 months after delivery; there were no clinically relevant drug-related safety findings in infants exposed to tenofovir disoproxil fumarate during late gestation. An imal Data TDF was administered orally to pregnant rats (at 0, 50, 150, or 450 mg/kg/day) and rabbits (at 0, 30, 100, or 300 mg/kg/day) through organogenesis (on gestation days 7 through 17, and 6 through 18, respectively).
No significant toxicological effects were observed in embryo-fetal toxicity studies performed with TDF in rats at doses up to 14 times the human dose based on body surface area comparisons and in rabbits at doses up to 19 times the human dose based on body surface area comparisons. In a pre/postnatal development study in rats, TDF was administered or…
🆘 Overdosage ▾
10 OVERDOSAGE 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 tablet, 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 TDF have been evaluated in healthy volunteers and HIV-1 infected individuals. Tenofovir pharmacokinetics are similar between these populations. Ab sorption Tenofovir disoproxil fumarate is 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 ± 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 dose range of 75 mg to 600 mg and are not affected by repeated dosing. In a single-dose bioequivalence study conducted under non-fasted conditions (dose administered with 4 oz. applesauce) in healthy adult volunteers, the mean C max of tenofovir was 26% lower for the oral powder relative to the tablet formulation. Mean AUC of tenofovir was similar between the oral powder and tablet formulations.
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 1.0 mg/kg and 3.0 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 tablet, 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. E ffects 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-∞ of approximately 40% and an increase in C max of approximately 14%. However, administration of tenofovir disoproxil fumarate 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. Specific Po p u lations 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. Ped iatric Patients Steady-state pharmacokinetics of tenofovir were evaluated in 31 HIV-1 infected pediatric subjects 2 years to less than 18 years of age (Table 13). Tenofovir exposure achieved in these pediatric subjects receiving oral once daily doses of tenofovir disoproxil fumarate 300 mg (tablet) was similar to exposures achieved in adults receiving once-daily doses of tenofovir disoproxil fumarate 300 mg.
Table 13 Mean (± SD)…
📦 How Supplied / Storage and Handling ▾
16 HOW SUPPLIED/STORAGE AND HANDLING Tenofovir disoproxil fumarate tablets, 300 mg, are light blue, oval shaped, film-coated tablet, debossed “CE 54” on one side, plain on the other side and containing 300 mg of tenofovir disoproxil fumarate, which is equivalent to 245 mg of tenofovir disoproxil. They are supplied as follows: Bottles of 30s (NDC 62135-466-30) Store tenofovir disoproxil fumarate tablets at 20°C to 25°C (68°F to 77°F), excursions permitted from 15°C to 30°C (59°F to 86°F) ( See USP Controlled Room Temperature ).
Keep the bottle tightly closed. Dispense only in original container. Do not use if seal over bottle opening is broken or missing.
📋 Description ▾
11 DESCRIPTION Tenofovir disoproxil fumarate tablets is the brand name for tenofovir disoproxil fumarate (TDF) (a prodrug of tenofovir) which is a fumaric acid salt of bis-isopropoxycarbonyloxymethyl ester derivative of tenofovir. TDF is converted in vivo to tenofovir, an acyclic nucleoside phosphonate (nucleotide) analog of adenosine 5’-monophosphate. Tenofovir exhibits activity against HIV-1 reverse transcriptase.
The chemical name of TDF 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 635.51 g/mol. It has the following structural formula: Tenofovir disoproxil fumarate is a white to off-white powder, slightly soluble in water.
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 in strength of 300 mg of TDF, which is equivalent to 245 mg of tenofovir disoproxil.
Each tablet contains the following inactive ingredients: anhydrous lactose, calcium stearate, colloidal silicon dioxide, crospovidone, FD&C Blue No. 2 lake 12 to 14%, polyethylene glycol, polyvinyl alcohol, talc, and titanium dioxide. In this insert, all dosages are expressed in terms of TDF except where otherwise noted. image description
💬 Information for Patients ▾
17 PATIENT COUNSELING INFORMATION Advise the patient to read the FDA-approved patient labeling ( Patient Information and Instructions for Use ). Severe Acute Exacerbation of Hepatitis B in Patients Infected with HBV Inform patients that severe acute exacerbations of hepatitis B have been reported in patients infected with hepatitis B virus (HBV) and have discontinued tenofovir disoproxil fumarate tablets. Advise patients not to discontinue tenofovir disoproxil fumarate tablets without first informing their healthcare provider.
All patients should be tested for HBV infection before or when starting tenofovir disoproxil fumarate tablets and those who are infected with HBV need close medical follow-up for several months after stopping tenofovir disoproxil fumarate tablets to monitor for exacerbations of hepatitis [see Warnings and Precautions ( 5.1 )] . New Onset or Worsening Renal Impairment Inform patients that renal impairment, including cases of acute renal failure and Fanconi syndrome, has been reported in association with the use of tenofovir disoproxil fumarate tablets.
Advise patients to avoid tenofovir disoproxil fumarate tablets with concurrent or recent use of a nephrotoxic agent (e.g., high-dose or multiple NSAIDs) [see Warnings and Precautions ( 5.2 )] . The dosing interval of tenofovir disoproxil fumarate tablets may need adjustment in HIV-1 infected patients with renal impairment. Immune Reconstitution Syndrome Inform patients that in some patients with advanced HIV infection (AIDS) 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 ( 5.4 )] . Bone Loss and Mineralization Defects Inform patients that decreases in bone mineral density have been observed with the use of tenofovir disoproxil fumarate tablets.
Consider bone monitoring in patients who have a history of pathologic bone fracture or at risk for osteopenia [see Warnings and Precautions ( 5.5 )]. Lactic Acidosis and Severe Hepatomegaly Inform patients that 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 ( 5.6 )] .
Drug Interactions Advise patients that tenofovir disoproxil fumarate tablets may interact with many drugs; therefore, advise patients to report to their healthcare provider the use of any other medication, including other HIV drugs and drugs for treatment of hepatitis C virus [see Warnings and Precautions ( 5.7 ) and Drug Interactions ( 7 )] . Dosing Recommendations Inform patients that it is important to take tenofovir disoproxil fumarate tablets on a regular dosing schedule with or without food and to avoid missing doses as it can result in development of resistance [see Dosage and Administration ( 2 )].
Pregnancy Registry Inform patients that there is an antiretroviral pregnancy registry to monitor fetal outcomes of pregnant women exposed to tenofovir disoproxil fumarate tablets [see Use in Specific Populations ( 8.1 )] . Lactation Instruct mothers not to breastfeed if they are taking tenofovir disoproxil fumarate tablets for the treatment of HIV-1 infection because of the risk of passing the HIV-1 virus to the baby [see Use in Specific Populations ( 8.2 )] . Treatment Duration Advise patients that 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. Manufactured For: Chartwell RX,…