Recommended Topic Related To:

Inlyta

"Investigators in The Cancer Genome Atlas (TCGA) Research Network have uncovered a connection between how tumor cells use energy from metabolic processes and the aggressiveness of the most common form of kidney cancer, clear cell renal cell carcin"...

Inlyta

SIDE EFFECTS

Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in clinical practice.

The safety of INLYTA has been evaluated in 715 patients in monotherapy studies, which included 537 patients with advanced RCC. The data described [see ADVERSE REACTIONS] reflect exposure to INLYTA in 359 patients with advanced RCC who participated in a randomized clinical study versus sorafenib [see Clinical Studies].

The following risks, including appropriate action to be taken, are discussed in greater detail in other sections of the label [see WARNINGS AND PRECAUTIONS]: hypertension, arterial thromboembolic events, venous thromboembolic events, hemorrhage, cardiac failure, gastrointestinal perforation and fistula formation, thyroid dysfunction, wound healing complications, RPLS, proteinuria, elevation of liver enzymes, hepatic impairment and fetal development.

Clinical Trials Experience

The median duration of treatment was 6.4 months (range 0.03 to 22.0) for patients who received INLYTA and 5.0 months (range 0.03 to 20.1) for patients who received sorafenib. Dose modifications or temporary delay of treatment due to an adverse reaction occurred in 199/359 patients (55%) receiving INLYTA and 220/355 patients (62%) receiving sorafenib. Permanent discontinuation due to an adverse reaction occurred in 34/359 patients (9%) receiving INLYTA and 46/355 patients (13%) receiving sorafenib.

The most common ( ≥ 20%) adverse reactions observed following treatment with INLYTA were diarrhea, hypertension, fatigue, decreased appetite, nausea, dysphonia, palmar-plantar erythrodysesthesia (hand-foot) syndrome, weight decreased, vomiting, asthenia, and constipation. Table 1 presents adverse reactions reported in ≥ 10% patients who received INLYTA or sorafenib.

Table 1: Adverse Reactions Occurring in ≥ 10% of Patients Who Received INLYTA or Sorafenib

Adverse Reactiona INLYTA
(N=359)
Sorafenib
(N=355)
All Gradesb % Grade 3/4 % All Gradesb % Grade 3/4 %
Diarrhea 55 11 53 7
Hypertension 40 16 29 11
Fatigue 39 11 32 5
Decreased appetite 34 5 29 4
Nausea 32 3 22 1
Dysphonia 31 0 14 0
Palmar-plantar erythrodysesthesia syndrome 27 5 51 16
Weight decreased 25 2 21 1
Vomiting 24 3 17 1
Asthenia 21 5 14 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
aPercentages are treatment-emergent, all-causality events
bNational Cancer Institute Common Terminology Criteria for Adverse Events, Version 3.0

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%), glossodynia (3%), pulmonary embolism (2%), rectal hemorrhage (2%), hemoptysis (2%), deep vein thrombosis (1%), retinal-vein occlusion/thrombosis (1%), polycythemia (1%), and transient ischemic attack (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 Gradesa% Grade 3/4 % All Gradesa % Grade 3/4 %
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
aNational Cancer Institute Common Terminology Criteria for Adverse Events, Version 3.0
ALP: alkaline phosphatase; ALT: alanine aminotransferase; AST: aspartate aminotransferase

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) and hypercalcemia (6% for INLYTA versus 2% for sorafenib).

Read the Inlyta (axitinib) Side Effects Center for a complete guide to possible side effects

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.

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 strong CYP3A4/5 inhibitors should be avoided. Grapefruit or grapefruit juice may also increase axitinib plasma concentrations and should be avoided. Selection of concomitant medication with no or minimal CYP3A4/5 inhibition potential is recommended. If a strong CYP3A4/5 inhibitor must be co-administered, the INLYTA dose should be reduced [see DOSAGE AND ADMINISTRATION and CLINICAL PHARMACOLOGY].

CYP3A4/5 Inducers

Co-administration of rifampin, a strong inducer of CYP3A4/5, reduced the plasma exposure of axitinib in healthy volunteers. Co-administration of INLYTA with strong CYP3A4/5 inducers (e.g., rifampin, dexamethasone, phenytoin, carbamazepine, rifabutin, rifapentin, phenobarbital, and St. John's wort) should be avoided. Selection of concomitant medication with no or minimal CYP3A4/5 induction potential is recommended [see DOSAGE AND ADMINISTRATION and CLINICAL PHARMACOLOGY]. Moderate CYP3A4/5 inducers (e.g., bosentan, efavirenz, etravirine, modafinil, and nafcillin) may also reduce the plasma exposure of axitinib and should be avoided if possible.

Read the Inlyta Drug Interactions Center for a complete guide to possible interactions

Last reviewed on RxList: 8/15/2014
This monograph has been modified to include the generic and brand name in many instances.

A A A

Additional Inlyta Information

Report Problems to the Food and Drug Administration

 

You are encouraged to report negative side effects of prescription drugs to the FDA. Visit the FDA MedWatch website or call 1-800-FDA-1088.


Women's Health

Find out what women really need.