The table below shows the effects of acid-reducing agents (protein pump inhibitors) on select kinase inhibitors, together with recommendations for coadministration. Click here to print these pages for use in the clinic.
Kinase inhibitor |
Recommendations |
Afatinib |
Tmax (hour): 2-5 PPI: N.A. Time of intake of kinase inhibitor and PPI: N.A. Effect on kinase inhibitor exposure - AUC: N.A. Effect on kinase inhibitor exposure - Cmax:N.A. (FDA/EMA) recommendations: PPIs can be used concomitantly* Refs.: 1,2 |
Axitinib |
Tmax (hour): 2-4 PPI: Rabeprazole 20mg q.d. Time of intake of kinase inhibitor and PPI: Concomitantly Effect on kinase inhibitor exposure - AUC: 15%¯ Effect on kinase inhibitor exposure - Cmax:42%¯ (FDA/EMA) recommendations: PPIs can be used concomitantly Refs.: 1,2 |
Bosutinib |
Tmax (hour): 6 PPI: Lansoprazole 60mg q.d., Time of intake of kinase inhibitor and PPI: Concomitantly Effect on kinase inhibitor exposure - AUC: 26%↓ Effect on kinase inhibitor exposure - Cmax:46%↓ (FDA/EMA) recommendations: Avoid combination Refs.: 3 |
Cabozantinib |
Tmax (hour): 2-5 PPI: Omeprazole 40 mg q.d. Time of intake of kinase inhibitor and PPI: PPI 1 hour before cabozantinib Effect on kinase inhibitor exposure - AUC: 7%↓ Effect on kinase inhibitor exposure - Cmax:10%↓ (FDA/EMA) recommendations: PPIs can be used concomitantly Refs.: 1,2 |
Crizotinib |
Tmax (hour): 4-6 PPI: Esomeprazole 40 mg Time of intake of kinase inhibitor and PPI: Concomitantly Effect on kinase inhibitor exposure - AUC: 10%↓ Effect on kinase inhibitor exposure - Cmax:-- (FDA/EMA) recommendations: PPIs can be used concomitantly Refs.: 1,2 |
Dabrafenib |
Tmax (hour): 2 PPI: N.a. Time of intake of kinase inhibitor and PPI: N.A. Effect on kinase inhibitor exposure - AUC: N.A. Effect on kinase inhibitor exposure - Cmax:N.A. (FDA/EMA) recommendations: Avoid combination* Refs.: 1,2 |
Dasatinib |
Tmax (hour): 0,5-3 PPI: Omeprazole 40mg q.d. Time of intake of kinase inhibitor and PPI: Concomitantly Effect on kinase inhibitor exposure - AUC: 43%↓ Effect on kinase inhibitor exposure - Cmax:42%↓ (FDA/EMA) recommendations: Avoid combination Refs.: 1,2,4 |
Erlotinib |
Tmax (hour): 4 PPI: Omeprazole 40mg q.d. Time of intake of kinase inhibitor and PPI: Concomitantly Effect on kinase inhibitor exposure - AUC: 46%↓ Effect on kinase inhibitor exposure - Cmax:61%↓ (FDA/EMA) recommendations: Avoid combination Refs.: 1,2 |
Gefitinib |
Tmax (hour): 3-7 PPI: N.A. Time of intake of kinase inhibitor and PPI: N.A. Effect on kinase inhibitor exposure - AUC: N.A. Effect on kinase inhibitor exposure - Cmax:N.A. (FDA/EMA) recommendations: Avoid combination** Refs.: 1,2 |
Ibrutinib |
Tmax (hour): 1-2 PPI: N.A. Time of intake of kinase inhibitor and PPI: N.A. Effect on kinase inhibitor exposure - AUC: N.A. Effect on kinase inhibitor exposure - Cmax:N.A. (FDA/EMA) recommendations: Avoid combination* Refs.: 1,2 |
Imatinib |
Tmax (hour): 2-4 PPI: Omeprazole 40mg q.d. Time of intake of kinase inhibitor and PPI: Concomitantly Effect on kinase inhibitor exposure - AUC: -- Effect on kinase inhibitor exposure - Cmax:-- (FDA/EMA) recommendations: PPIs can be used concomitantly Refs.: 1,2 |
Lapatinib |
Tmax (hour): 3-4 PPI: Esomeprazole 40mg q.d. Time of intake of kinase inhibitor and PPI: PPI 12 hours before Lapatinib Effect on kinase inhibitor exposure - AUC: 27%↓ Effect on kinase inhibitor exposure - Cmax:-- (FDA/EMA) recommendations: Avoid combination Refs.: 1,2 |
Nilotinib |
Tmax (hour): 3 PPI: Esomeprazole 40mg q.d. Time of intake of kinase inhibitor and PPI: Concomitantly Effect on kinase inhibitor exposure - AUC: 34%↓ Effect on kinase inhibitor exposure - Cmax:27%↓ (FDA/EMA) recommendations: PPIs can be used concomitantly Refs.: 5-7 |
Nintedanib |
Tmax (hour): 2-4 PPI: N.A. Time of intake of kinase inhibitor and PPI: N.A. Effect on kinase inhibitor exposure - AUC: N.A. Effect on kinase inhibitor exposure - Cmax:N.A. (FDA/EMA) recommendations: PPIs can be used concomitantly* Refs.: 1,2 |
Pazopanib |
Tmax (hour): 3,5 PPI: Esomeprazole 40 mg q.d. Time of intake of kinase inhibitor and PPI: Concomitantly*** Effect on kinase inhibitor exposure - AUC: 40%↓ Effect on kinase inhibitor exposure - Cmax:42%↓ (FDA/EMA) recommendations: PPIs can be used concomitantly Refs.: 1,2 |
Ponatinib |
Tmax (hour): 4 PPI: Lansoprazole 60mg q.d. Time of intake of kinase inhibitor and PPI: Concomitantly Effect on kinase inhibitor exposure - AUC: -- Effect on kinase inhibitor exposure - Cmax:25%↓ (FDA/EMA) recommendations: PPIs can be used concomitantly Refs.: 8 |
Regorafenib |
Tmax (hour): 3-4 PPI: N.A. Time of intake of kinase inhibitor and PPI: N.A. Effect on kinase inhibitor exposure - AUC: N.A. Effect on kinase inhibitor exposure - Cmax:N.A. (FDA/EMA) recommendations: Avoid combination Refs.: 1,2 |
Ruxolitinib |
Tmax (hour): 1 PPI: N.A. Time of intake of kinase inhibitor and PPI: N.A. Effect on kinase inhibitor exposure - AUC: N.A. Effect on kinase inhibitor exposure - Cmax:N.A. (FDA/EMA) recommendations: PPIs can be used concomitantly* Refs.: 1,2 |
Sorafenib |
Tmax (hour): 3 PPI: Esomeprazole 40 mg q.d. Time of intake of kinase inhibitor and PPI: Concomitantly Effect on kinase inhibitor exposure - AUC: -- Effect on kinase inhibitor exposure - Cmax:-- (FDA/EMA) recommendations: PPIs can be used concomitantly Refs.: 1,2 |
Sunitinib |
Tmax (hour): 6-12 PPI: N.A. Time of intake of kinase inhibitor and PPI: N.A. Effect on kinase inhibitor exposure - AUC: N.A. Effect on kinase inhibitor exposure - Cmax:N.A. (FDA/EMA) recommendations: PPIs can be used concomitantly* Refs.: 1,2 |
Trametinib |
Tmax (hour): 1,5 PPI: N.A. Time of intake of kinase inhibitor and PPI: N.A. Effect on kinase inhibitor exposure - AUC: N.A. Effect on kinase inhibitor exposure - Cmax:N.A. (FDA/EMA) recommendations: PPIs can be used concomitantly* Refs.: 1,2 |
Vandetanib |
Tmax (hour): 6 PPI: Omeprazole 40 mg q.d. Time of intake of kinase inhibitor and PPI: Concomitantly Effect on kinase inhibitor exposure - AUC: -- Effect on kinase inhibitor exposure - Cmax:15%↓ (FDA/EMA) recommendations: PPIs can be used concomitantly Refs.: 9 |
Vemurafenib |
Tmax (hour): 4 PPI: N.A. Time of intake of kinase inhibitor and PPI: N.A. Effect on kinase inhibitor exposure - AUC: N.A. Effect on kinase inhibitor exposure - Cmax:N.A. (FDA/EMA) recommendations: PPIs can be used concomitantly* Refs.: 1,2 |
* Based only on “in vitro” and basic chemical data; ** Based on a study with ranitidine 450mg bid., 13 hours and 1 hour before gefitinib (AUC 47%↓; Cmax 71%↓); *** Esomeprazole (evening) concomitantly with pazopanib (in the morning).