3
Constipation
20
1
20
1
Hypothyroidism
19
<1
8
0
Cough
15
1
17
1
Mucosal inflammation
15
1
12
1
Arthralgia
15
2
11
1
Stomatitis
15
1
12
<1
Dyspnea
15
3
12
3
Abdominal pain
14
2
11
1
Headache
14
1
11
0
Pain in extremity
13
1
14
1
Rash
13
<1
32
4
Proteinuria
11
3
7
2
Dysgeusia
11
0
8
0
Dry skin
10
0
11
0
Dyspepsia
10
0
2
0
Pruritus
7
0
12
0
Alopecia
4
0
32
0
Erythema
2
0
10
<1
Selected adverse reactions (all grades) that were reported in <10% of patients treated with INLYTA included dizziness (9%), upper abdominal pain (8%), myalgia (7%), dehydration (6%), epistaxis (6%), anemia (4%), hemorrhoids (4%), hematuria (3%), tinnitus (3%), lipase increased (3%), pulmonary embolism (2%), rectal hemorrhage (2%), hemoptysis (2%), deep vein thrombosis (1%), retinal-vein occlusion/thrombosis (1%), polycythemia (1%), transient ischemic attack (1%), and RPLS (<1%).
Table 2 presents the most common laboratory abnormalities reported in ≥10% patients who received INLYTA or sorafenib.
Table 2. Laboratory Abnormalities Occurring in ≥10% of Patients Who Received INLYTA or Sorafenib
Laboratory Abnormality
N
INLYTA
N
Sorafenib
All Grades*
Grade 3/4
All Grades*
Grae 3/4
%
%
%
%
ALP: alkaline phosphatase; ALT: alanine aminotransferase; AST: aspartate aminotransferase
* National Cancer Institute Common Terminology Criteria for Adverse Events, Version 3.0
Hematology
Hemoglobin decreased
320
35
<1
316
52
4
Lymphocytes (absolute) decreased
317
33
3
309
36
4
Platelets decreased
312
15
<1
310
14
0
White blood cells decreased
320
11
0
315
16
<1
Chemistry
Creatinine increased
336
55
0
318
41
<1
Bicarbonate decreased
314
44
<1
291
43
0
Hypocalcemia
336
39
1
319
59
2
ALP increased
336
30
1
319
34
1
Hyperglycemia
336
28
2
319
23
2
Lipase increased
338
27
5
319
46
15
Amylase increased
338
25
2
319
33
2
ALT increased
331
22
<1
313
22
2
AST increased
331
20
<1
311
25
1
Hypernatremia
338
17
1
319
13
1
Hypoalbuminemia
337
15
<1
319
18
1
Hyperkalemia
333
15
3
314
10
3
Hypoglycemia
336
11
<1
319
8
<1
Hyponatremia
338
13
4
319
11
2
Hypophosphatemia
336
13
2
318
49
16
Selected laboratory abnormalities (all grades) that were reported in <10% of patients treated with INLYTA included hemoglobin increased (above the upper limit of normal) (9% for INLYTA versus 1% for sorafenib).
7 DRUG INTERACTIONS
In vitro data indicate that axitinib is metabolized primarily by CYP3A4/5 and, to a lesser extent, CYP1A2, CYP2C19, and uridine diphosphate-glucuronosyltransferase (UGT) 1A1.
7.1 CYP3A4/5 Inhibitors
Co-administration of ketoconazole, a strong inhibitor of CYP3A4/5, increased the plasma exposure of axitinib in healthy volunteers. Co-administration of INLYTA with |
