SPL Set ID: 7bf86d9d-999a-4b64-849a-0d43bbf7b766

Emtricitabine and tenofovir disoproxil fumarate tablets are fixed-dose combination tablets containing emtricitabine (FTC) and tenofovir disoproxil fumarate (TDF). FTC is a synthetic nucleoside analog of cytidine. TDF is converted in vivo to tenofovir, an acyclic nucleoside phosphonate (nucleotide) analog of adenosine 5′-monophosphate. Both FTC and tenofovir exhibit inhibitory activity against HIV-1 reverse transcriptase. Emtricitabine: The chemical name of FTC is 4-Amino-5-fluoro-1-[(2 R ,5 S )-2-(hydroxylmethyl)-1,3-oxathiolan-5-yl]-2(1 H )-pyrimidinone. FTC is the (-) enantiomer of a thio analog of cytidine, which differs from other cytidine analogs in that it has a fluorine in the 5-position. It has a molecular formula of C 8 H 10 FN 3 O 3 S and a molecular weight of 247.30. It has the following structural formula: FTC is a white to almost white crystalline powder with a solubility of approximately 100 mg/mL in water at 25°C. The partition coefficient (log p) for emtricitabine is −1.07 and the pKa is 2.27. Tenofovir Disoproxil Fumarate: TDF is a fumaric acid salt of the bis-isopropoxycarbonyloxymethyl ester derivative of tenofovir. The chemical name of tenofovir DF is 9-[( R )-2-[[bis(isopropoxycarbonyl)oxy]methoxy]phosphinyl]methoxy]propyl]adenine fumarate. 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 disoproxil fumarate is a white to off white powder soluble in methanol, slightly soluble in water. The partition coefficient (log p) for tenofovir disoproxil is 0.75 and the pKa is 3.95. All dosages are expressed in terms of TDF except where otherwise noted. Emtricitabine and Tenofovir Disoproxil Fumarate Tablets are for oral administration, and are available in the following strength: Film-coated tablet containing emtricitabine 200 mg and tenofovir disoproxil fumarate 300 mg equivalent to tenofovir disoproxil 245 mg as active ingredients Emtricitabine and Tenofovir Disoproxil Fumarate Tablets also include the following inactive ingredients: croscarmellose sodium, lactose anhydrous, magnesium stearate, and microcrystalline cellulose. The tablets are coated with Opadry II White 32K580000, which contains hypromellose 2910, lactose monohydrate, titanium dioxide, and triacetin. Emtricitabine Structure Tenofovir Disoproxil Fumarate Structure