SPL Set ID: 974d2ec8-1b51-4e69-991d-0d5dea8360f4

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 5-fluoro-1-(2 R ,5 S )-[2-(hydroxymethyl)-1,3-oxathiolan-5-yl]cytosine. 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 247.24. It has the following structural formula: FTC is a white to off-white powder with a solubility of approximately 112 mg/mL in water at 25ºC. The partition coefficient (log p) for emtricitabine is -0.43 and the pKa is 2.65. 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 (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 disoproxil fumarate is a white to off-white crystalline powder with a solubility of 13.4 mg/mL in water at 25ºC. The partition coefficient (log p) for tenofovir disoproxil is 1.25 and the pKa is 3.75. 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 strengths: Film-coated tablet containing 167 mg of FTC and 250 mg of TDF (which is equivalent to 204 mg of tenofovir disoproxil) as active ingredients Film-coated tablet containing 133 mg of FTC and 200 mg of TDF (which is equivalent to 163 mg of tenofovir disoproxil) as active ingredients Film-coated tablet containing 100 mg of FTC and 150 mg of TDF (which is equivalent to 123 mg of tenofovir disoproxil) as active ingredients All strengths of emtricitabine and tenofovir disoproxil fumarate tablets also include the following inactive ingredients: croscarmellose sodium, hypromellose, lactose monohydrate, magnesium stearate, microcrystalline cellulose, pregelatinized starch (maize), titanium dioxide and triacetin. structure1 structure2