KRINTAFEL

AbsorptionMaximum plasma concentrations were generally observed 12 to 15 hours following oral administration. Food Effect: Plasma tafenoquine AUC increased by 41% and C max increased by 31% when administered as an investigational capsule formulation with a high-calorie, high-fat meal (approximately 1,000 calories with 15% protein, 25% carbohydrate, and 60% fat) compared with the fasted state.

DistributionProtein binding of tafenoquine is >99.5%. The apparent oral volume of distribution is ~1,6...

Trial 1(NCT01376167) was a double-blind, controlled clinical trial of 522 adults positive for P. vivax across 3 regions (Asia, Africa, and Latin America). All patients received chloroquine phosphate (600-mg free base on Days 1 and 2 with 300-mg free base on Day 3) to treat the acute infection in addition to either a one-time dose of KRINTAFEL (two 150-mg tablets) on Day 1 or Day 2 (n = 260), an active control (n = 129), or placebo (n = 133) in a 2:1:1 fashion. Patients included in the trial had a mean age of 35 (range: 16 to 79 years), were 75% male and from the following regions: 70% Latin A...

The following clinically significant adverse reactions have been observed with KRINTAFEL and are discussed in detail in the Warnings and Precautions section:

• Hemolytic anemia [see Warnings and Precautions ( 5.1 )]
• Methemoglobinemia [see Warnings and Precautions ( 5.3 )]
• Psychiatric effects [see Warnings and Precautions ( 5.4 )]
• Hypersensitivity reactions [see Warnings and Precautions ( 5.5 )] Common adverse reactions (≥5%) were dizziness, nausea, vomiting, headache, and decreased hemoglo...

KRINTAFEL is contraindicated in:

• Patients with G6PD deficiency or unknown G6PD status due to the risk of hemolytic anemia [see Warnings and Precautions ( 5.1 )] .
• Breastfeeding by a lactating woman when the infant is found to be G6PD deficient or if the G6PD status of the infant is unknown [see Use in Specific Populations ( 8.2 )].
• Patients with known hypersensitivity to tafenoquine, other 8...

• Hemolytic Anemia : G6PD testing must be performed before prescribing KRINTAFEL due to the risk of hemolytic anemia. Monitor patients for clinical signs or symptoms of hemolysis. ( 5.1 )
• G6PD Deficiency in Pregnancy or Lactation : KRINTAFEL may cause hemolytic anemia when administered to a pregnant woman with a G6PD-deficient fetus. KRINTAFEL is not recommended during pregnancy. A G6PD-deficient infant may be at risk for hemolytic anemia from exposure to KRINTAFEL through breast milk. Check i...

7 DRUG INTERACTIONS Avoid coadministration with drugs that are substrates of organic cation transporter-2 (OCT2) or multidrug and toxin extrusion (MATE) transporters. ( 7.1 ) 7.1 Effect of KRINTAFEL on Organic Cation Transporter-2 (OCT2) and Multidrug and Toxin Extrusion (MATE) Substrates The effect of coadministration of tafenoquine on the pharmacokinetics of OCT2 and MATE substrates in humans is...