INLYTA*
Manufacturer DetailsGENERIC*
USA AND CANADA
Compositions:
Axitinib- mg,
Axitinib- mg,
| Strength | Rate | Packing Style |
|---|---|---|
| mg | 0.00 | unit |
List of Related Indications:
- Treatment of adult patients with advanced kidney cancer(renal call carcinoma) who have not responded to another drug for this type of cancer
List Of Drugs:
- Axitinib- Inlyta (Jan 2012) and Tabs (Sep 2014)- Chemotherapeutic Agent
Indication Type Description:
Drug Interaction
Indication
Adverse Reaction
Contra-Indications
Dosages/ Overdosage Etc
Patient Information
Pharmacology/ Pharmacokinetics
Pregnancy and lactation
Drug Interaction:
Avoid strong CYP3A4/5 inhibitors. If unavoidable, reduce the INLYTA dose.
Avoid strong CYP3A4/5 inducers.
Indication:
NLYTA® (axitinib) tablets for oral administration
Initial U.S. Approval: 2012
Drug Name- Inlyta
Active Ingredient - Axitinib
To treat patients with advanced kidney cancer (renal cell carcinoma)
who have not responded to another drug for this type of cancer
Indication-
To treat patients with advanced kidney cancer (renal cell carcinoma)
who have not responded to another drug for this type of cancer
Approved by FDA on 27-1-2012 (Ref- FDA Approved List- 2012)
Axitinib tablet 1mg/5mg
Indication-
For the treatment of advanced renal cell carcinoma after failure of one prior
systemic therapy
Approved by FDA on 18-09-2014 (Ref- FDA approved List- 2014)
New drugs approved For Marketing by Drug Controller General of India(DCGI )
during the period January 1988 to November 2014
(Ref- IDMA Annual Publication 2015)
Name of Drug Indication Date of Approval
Axitinib tablet 1mg/5mg 18-09-2014
For the treatment of advanced renal cell carcinoma after
failure of one prior systemic therapy
Adverse Reaction:
The most common (.20%) adverse reactions are diarrhea, hypertension, fatigue,
decreased appetite, nausea, dysphonia, palmar-plantar erythrodysesthesia
(hand-foot) syndrome, weight decreased, vomiting, asthenia, and constipation.
Contra-Indications:
CONTRAINDICATIONS
None
WARNINGS AND PRECAUTIONS
Hypertension including hypertensive crisis has been observed. Blood
pressure should be well-controlled prior to initiating INLYTA.
Monitor for hypertension and treat as needed. For persistent hypertension
despite use of anti-hypertensive medications, reduce the INLYTA dose.
Arterial and venous thrombotic events have been observed and can be fatal.
Use with caution in patients who are at increased risk for these events.
Hemorrhagic events, including fatal events, have been reported. INLYTA has
not been studied in patients with evidence of untreated brain metastasis
or recent active gastrointestinal bleeding and should not be used
in those patients. )
Gastrointestinal perforation and fistula, including death, have occurred.
Use with caution in patients at risk for gastrointestinal perforation or fistula.
Hypothyroidism requiring thyroid hormone replacement has been reported.
Monitor thyroid function before initiation of, and periodically throughout
, treatment with INLYTA.
Stop INLYTA at least 24 hours prior to scheduled surgery.
Reversible Posterior Leukoencephalopathy Syndrome (RPLS) has been
observed. Permanently discontinue INLYTA if signs or symptoms of RPLS occur.
Monitor for proteinuria before initiation of, and periodically throughout, treatment
with INLYTA. For moderate to severe proteinuria, reduce the dose or temporarily
interrupt treatment with INLYTA.
Liver enzyme elevation has been observed during treatment with INLYTA.
Monitor ALT, AST and bilirubin before initiation of, and periodically throughout,
treatment with INLYTA.
The starting dose of INLYTA should be decreased if used in patients with
moderate hepatic impairment. INLYTA has not been studied in patients with
severe hepatic impairment.
INLYTA can cause fetal harm when administered to a pregnant woman based
on its mechanism of action. Women of childbearing potential should be advised
of the potential hazard to the fetus and to avoid becoming pregnant while
receiving INLYTA.
Dosages/ Overdosage Etc:
Indication-
For the treatment of advanced renal cell carcinoma after failure of one prior
systemic therapy
INDICATIONS AND USAGE
INLYTA is a kinase inhibitor indicated for the treatment of advanced renal cell
carcinoma after failure of one prior systemic therapy.
DOSAGE AND ADMINISTRATION
The starting dose is 5 mg orally twice daily. Dose adjustments can be made
based on individual safety and tolerability.
Administer INLYTA dose approximately 12 hours apart with or without food.
INLYTA should be swallowed whole with a glass of water.
If a strong CYP3A4/5 inhibitor is required, decrease the INLYTA dose by
approximately half.
For patients with moderate hepatic impairment, decrease the starting dose
by approximately half.
DOSAGE FORMS AND STRENGTHS
3 mg and 5 mg tablets
Patient Information:
PATIENT COUNSELING INFORMATION
See FDA-approved patient labeling
1. Hypertension
Advise patients that hypertension may develop during INLYTA treatment and that
blood pressure should be monitored regularly during treatment
.
2. Arterial/Venous Thromboembolic Events
Advise patients that arterial and venous thromboembolic events have been
observed during INLYTA treatment and to inform their doctor if they experience
symptoms suggestive of thromboembolic events
3. Hemorrhage
Advise patients that INLYTA may increase the risk of bleeding and to promptly
inform their doctor of any bleeding episodes
4. Gastrointestinal Disorders
Advise patients that gastrointestinal disorders such as diarrhea, nausea, vomiting,
and constipation may develop during INLYTA treatment and to seek immediate
medical attention if they experience persistent or severe abdominal pain
because cases of gastrointestinal perforation and fistula have been reported
in patients taking INLYTA
5. Abnormal Thyroid Function
Advise patients that abnormal thyroid function may develop during INLYTA
treatment and to inform their doctor if symptoms of abnormal thyroid function
occur.
6. Wound Healing Complications
Advise patients to inform their doctor if they have an unhealed wound or if they
have surgery scheduled
7. Reversible Posterior Leukoencephalopathy Syndrome
Advise patients to inform their doctor if they have worsening of neurological
function consistent with RPLS (headache, seizure, lethargy, confusion, blindness
and other visual and neurologic disturbances)
8. Pregnancy
Advise patients that INLYTA may cause birth defects or fetal loss and that they
should not become pregnant during treatment with INLYTA. Both male and female
patients should be counseled to use effective birth control during treatment
with INLYTA. Female patients should also be advised against breast-feeding
while receiving INLYTA
9. Concomitant Medications
Advise patients to inform their doctor of all concomitant medications, vitamins,
or dietary and herbal supplements.
Pharmacology/ Pharmacokinetics:
CLINICAL PHARMACOLOGY
1 Mechanism of Action
Axitinib has been shown to inhibit receptor tyrosine kinases including vascular
endothelial growth factor receptors (VEGFR)-1, VEGFR-2, and VEGFR-3
at therapeutic plasma concentrations.
These receptors are implicated in pathologic angiogenesis, tumor growth,
and cancer progression. VEGF-mediated endothelial cell proliferation
and survival were inhibited by axitinib in vitro and in mouse models.
Axitinib was shown to inhibit tumor growth and phosphorylation of VEGFR-2 in
tumor xenograft mouse models.
2. Pharmacokinetics
The population pharmacokinetic analysis pooled data from 17 trials in healthy subjects
and patients with cancer. A two-compartment disposition model with first-order absorption
and lag-time adequately describes the axitinib concentration-time profile.
Absorption and Distribution:
Following single oral 5-mg dose administration, the median Tmax ranged
from 2.5 to 4.1 hours. Based on the plasma half-life, steady state is expected
within 2 to 3 days of dosing. Dosing of axitinib at 5 mg twice daily
resulted in approximately 1.4-fold accumulation compared to administration
of a single dose.
At steady state, axitinib exhibits approximately linear pharmacokinetics
within the 1-mg to 20-mg dose range.
The mean absolute bioavailability of axitinib after an oral 5 mg dose is 58%.
Pregnancy and lactation:
USE IN SPECIFIC POPULATIONS
1. Pregnancy
Pregnancy Category D
There are no adequate and well-controlled studies with INLYTA in pregnant
women. INLYTA can cause fetal harm when administered to a pregnant woman
based on its mechanism of action.
If this drug is used during pregnancy, or if the patient becomes pregnant while
receiving this drug, the patient should be apprised of the potential hazard to the fetus.
2. Nursing Mothers
It is not known whether axitinib is excreted in human milk. Because many drugs are
excreted in human milk and because of the potential for serious adverse reactions
in nursing infants from INLYTA, a decision should be made whether to discontinue
nursing or to discontinue the drug, taking into account the importance of the drug
to the mother.
3. Pediatric Use
The safety and efficacy of INLYTA in pediatric patients have not been studied.
. Abnormalities in growing incisor teeth (including dental caries, malocclusions
and broken and/or missing teeth) were observed in mice administered
oral axitinib twice daily at .5 mg/kg/dose (approximately 1.5 times the
AUC in patients at the recommended starting dose).
4. Geriatric Use
In a controlled clinical study with INLYTA for the treatment of patients with RCC,
123/359 patients (34%) treated with INLYTA were .65 years of age.
Although greater sensitivity in some older individuals cannot be ruled out,
no overall differences were observed in the safety and effectiveness of
INLYTA between patients who were .65 years of age and younger.
No dosage adjustment is required in elderly patients].
