Krintafel

KRINTAFEL contains tafenoquine succinate, an antimalarial agent for oral administration. The chemical name of tafenoquine succinate is (±) 8-[(4-amino-1-methylbutyl)amino]-2,6dimethoxy-4-methyl-5-[3-(trifluoromethyl)phenoxy]quinoline succinate. The molecular formula of tafenoquine succinate is C24H28F3N3O3 • C4H6O4, and its molecular mass is 581.6 as the succinate salt (463.5 as free base). The structural formula is shown below.

Each KRINTAFEL tablet contains 150 mg of tafenoquine (equivalent to 188.2 mg tafenoquine succinate). Inactive ingredients include magnesium stearate, mannitol, and microcrystalline cellulose. The tablet film-coating inactive ingredients include hydroxypropylmethylcellulose, polyethylene glycol, red iron oxide, and titanium dioxide.

KRINTAFEL is indicated for the radical cure (prevention of relapse) of Plasmodium vivax malaria in patients aged 16 years and older who are receiving appropriate antimalarial therapy for acute P. vivax infection [see DOSAGE AND ADMINISTRATION].

Limitation Of Use

KRINTAFEL is NOT indicated for the treatment of acute P. vivax malaria.

Dosage Forms And Strengths

KRINTAFEL tablets are pink, film-coated, capsule-shaped tablets debossed with 'GS J11' on one side and contain 150 mg of tafenoquine.

Storage And Handling

KRINTAFEL tablets contain 150 mg of tafenoquine (equivalent to 188.2 mg tafenoquine succinate) and are pink, film-coated, capsule-shaped, and debossed with 'GS J11' on one side. KRINTAFEL is supplied as follows:

Bottle of 30 tablets with child-resistant closure (NDC 0173-0889-13). Bottles contain a desiccant. Once opened, use within 3 months.

Unit Dose Pack of 2 tablets in a bottle with child-resistant closure (NDC 0173-0889-39). Bottles contain a desiccant.

Store at 20°C to 25°C (68°F to 77°F). Temperature excursions are permitted to 15°C to 30°C (59°F to 86°F) [see USP Controlled Room Temperature].

Store in the original package to protect from moisture. Keep the bottle tightly closed and do not remove the desiccant.

GlaxoSmithKline Research Triangle Park, NC 27709. Revised: Jul 2018

Included as part of the PRECAUTIONS section.

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]
• Methemoglobinemia [see WARNINGS AND PRECAUTIONS]
• Psychiatric effects [see WARNINGS AND PRECAUTIONS]
• Hypersensitivity reactions [see WARNINGS AND PRECAUTIONS]

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 with rates in the clinical trials of another drug and may not reflect the rates observed in practice.

The safety data described below reflect exposure to 4,129 subjects, of whom 810 received a 300mg single dose of KRINTAFEL. KRINTAFEL was evaluated in patients with P. vivax malaria (n = 483) in 3 randomized, double-blind trials including a placebo-controlled trial comparing KRINTAFEL plus chloroquine (n = 260) with chloroquine alone (Trial 1), a placebo-controlled dose-ranging trial (Trial 2) (n = 57) [see Clinical Studies], and a hematologic safety trial (Trial 3, NCT02216123) (n = 166).

In Trial 1, in patients with P. vivax malaria, the most common adverse reactions reported in ≥5% of patients treated with KRINTAFEL are listed in Table 1. 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 America (Brazil and Peru), 19% Southeast (SE) Asia (Thailand, Cambodia, and the Philippines), and 11% Africa (Ethiopia).

Table 1: Selected Adverse Reactionsa Reported in ≥5% of Patients with P. Vivax Malaria Receiving KRINTAFEL in a Randomized, Active-Controlled Trial (Trial 1)

Clinically significant adverse reactions with KRINTAFEL 300-mg single dose in clinical trials (n = 810) in ≤3% of subjects are listed below:

Psychiatric Disorders: Anxiety, insomnia, abnormal dreams.

Nervous System Disorders: Somnolence.

Laboratory Investigations: Increased blood creatinine, increased blood methemoglobin, increased alanine aminotransferase.

Immune System Disorders: Hypersensitivity reactions (e.g., angioedema, urticaria) [see CONTRAINDICATIONS, WARNINGS AND PRECAUTIONS].

Eye Disorders: Vortex keratopathy, photophobia.

Read the entire FDA prescribing information for Krintafel (Tafenoquine Tablets)