In 2019, Turalio (Turalio is the brand name while Pexidartinib is the compound name) was FDA-approved with the recommended dose of 400 mg orally taken twice daily on an empty stomach for at least 1 hour before and 2 hours after a meal or snack (1). Prior to 2023, the total daily dose of Turalio taken by patients was 800 mg. Turalio came in 200 mg capsules.
Prior recommendations
However, in 2023, a study was conducted to determine the optimal dosing for Turalio leading to the changed recommendations (2). As of Feb 2023, the current recommended dosing for Turalio is 250 mg orally taken twice daily with a low-fat meal (approximately 11-14 g of total fat).
2023 Recommendations
No fast is required. However, according to studies conducted, when a high-fat meal (55-65g of total fat) is consumed, patients should wait >3 hours before taking Turalio with a low-fat meal. After a patient takes their Turalio with a low-fat meal, they should wait >2 hours before consuming a high-fat meal. There is no recommendation for fasting before or after a low-fat meal or medium-fat meal.
The total daily dose of Turalio taken by patients is 500 mg. Turalio comes in 125 mg capsules. Dose modifications are available for those who are not on the full dose (250 mg twice daily for a total of 500 mg). For example, the modified doses include 375 mg (one capsules in the morning and two capsule in the evening) or 250 mg (one capsule in the morning and one capsule in the evening) with a low-fat snack, respectively. This change in the dosing was made due to something called the Food Effect.
Food effect
Medication taken orally must go through the gut/stomach. Medications are taken based on food composition or on an empty stomach because food can influence the absorption of medicine. It is important to investigate the impact of food on the circulating medicine in the blood (medication within the body capable of having an effect) to accordingly adapt the dose, frequency of administration, and food conditions to optimize the treatment effectiveness and safety.
Fat in food can increase the absorption of the drug, potentially leading to harmful side effects. Food can also be used to reduce side effects and improve safety (example: certain antibiotics). In the case of Turalio, taking it on an empty stomach requires more drug within the capsule to get into the body and blood circulation. Previously, patients who ate too soon before or after taking Turalio (400mg twice daily) had potential for too much of the drug to be absorbed and providers had a concern for severe side effects if patients didn’t take it as prescribed. Therefore, a study was conducted to determine the best condition for patients to take Turalio. Food conditions (low-fat meal, medium-fat meal, and high-fat meal) were tested to optimize the safety and effectiveness of Turalio. It was found that 250 mg of Turalio taken twice daily (total 500 mg daily) with a low-fat meal was safe while maintaining the maximal anti-tumor effect because fat increased the absorption into body from the gut. However, when the same 250 mg of Turalio taken twice daily was consumed with a high-fat meal, potentially dangerous concentrations of the drug got into the blood. Therefore, Daiichi Sankyo, the drug company, determined that the best way to take Turalio is 250 mg twice daily (total 500 mg daily) with a low-fat meal. A low-fat meal is defined as 11-14 total grams of fat. The fat content, and not the total number of calories, is the most important factor in regards to the absorption of turalio.
Tips for taking Turalio from Healthcare Providers: - Take it at approximately the same time morning and night. - If a patient is unsure of the fat content of their meal, consider skipping the current dose and taking the next scheduled dose (Turalio has a long half-life in the body, giving some leeway with respect to timing). - Use regular snacks or meals that fulfill the fat requirement to remain consistent. - Dinner is the most variable meal of the day. Consider taking with a snack after dinner instead. - A food diary could be useful for finding the time of day and foods convenient for taking with Turalio. - Ask to see a dietitian if feasible to help guide foods that would fit into the fat requirement.
Discuss with your healthcare provider or pharmacy about these changes. A dietitian can provide additional assistance.
patient examples of low-fat Meal (11-14 G TOTAL FAT)
A spoonful of peanut butter
1.5 teaspoon of peanut butter and celery or banana (12 g)
1 teaspoon of peanut butter and 6 Ritz crackers (14 g)
Two hard-boil eggs (11 g)
1/3 cup of shredded cheese (12 g)
1/2 cup of hummus with veggies (12 g)
tortilla chips (approximately 10 chips) and salsa (11 g)
1/2 avocado and x2 toast (13 g)
1 Oz of cashews, pistachios, and/or almonds (24 almonds)
5 snack size Hershey bars with fruit
ranch dressing (< 2 teaspoons) and veggies (12 g)
1/2 cup of sunflower seeds (12 g)
1 teaspoon of butter melted on 1 piece of whole grain toast (13 g)
10 slices of pepperoni (11 g)
4 pieces of bacon (13 g)
1.5 cup of edamame (12 g)
7.25 oz of Mac and Cheese (12 g)
4 slices of salami (12 g)
1.25 slices of cheddar cheese (12 g)
2 peanut butter cookies (14 g)
2 slices of Swiss cheese (14 g)
16 Oz Soy milk (11 g)
1.5 cup of cottage cheese (13.5 g)
2 cups diced Turkey meat (light and dark meat) (14 g)
4 Oz of baked or broiled salmon (12 g)
6 Oz lean sirloin steak (12 g)
These examples of total grams of fat are approximate. Send in your examples to [email protected]
Patient Examples of Low-Fat Meals/Snacks (March 2023)
What are the dose modifications?
Patients who do not tolerate the maximum total daily dose (800 mg before Feb 2023 or 500 mg after Feb 2023) may receive dose modifications. These dose modifications are used to reduce side effects and improve tolerability.
For patients on Turalio before Feb 2023, the 400 mg and 600 mg dose modifications are equivalent to the 250 mg and 375mg, respectively, in the new label (see below). These modifications can be found on the packet insert or label.
