Skip to main content

Table 1 Physicochemical properties of imatinib, nilotinib and sunitinib

From: Effect of gastrointestinal resection on sunitinib exposure in patients with GIST

Drug

MW (g/mol)

pKa

Solubility

BCS class

Reference

Imatinib

493.60

7.7

Freely soluble (100–1000 mg/ml) up to pH 5.5. Solubility declines at higher pH; lowest solubility is 1 mg/ml.

II

[11]

Nilotinib

565.98

2.1 and 5.4

Slightly soluble (1–10 mg/ml) at pH 1.0, very slightly soluble (0.1-1 mg/ml) in water, at pH 3.0 and 3.0. Practically insoluble (<0.1 mg/ml) in buffer solutions of pH ≥ 4.5

IV

[12]

Sunitinib

398.47

9.0

25 mg/ml at pH 1.2-6.8. Solubility reduces at pH ≥ 6.8

IV

[16]

  1. Abbreviation: BCS Biopharmaceutics Classification System, MW molecular weight.