pharmacopeia
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/api/v1/drug/axitinib

Mechanism of action

Sourced from openFDA

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.

Receptor Tyrosine Kinase

Indications

Sourced from openFDA
  • INLYTA is a kinase inhibitor indicated: • in combination with avelumab, for the first-line treatment of patients with advanced renal cell carcinoma (RCC). ( 1.1 ) • in combination with pembrolizumab, for the first-line treatment of patients with advanced RCC.

Contraindications

Sourced from openFDA
  • None. None.contraindicated

Dosage & administration

Sourced from openFDA

• INLYTA 5 mg orally twice daily with avelumab 800 mg every 2 weeks. ( 2.1 ) • INLYTA 5 mg orally twice daily with pembrolizumab 200 mg every 3 weeks or 400 mg every 6 weeks. ( 2.1 ) • INLYTA as a single agent the starting dose is 5 mg orally twice daily. ( 2.1 ) • Dose adjustments can be made based on individual safety and tolerability. ( 2.2 ) • Administer INLYTA dose approximately 12 hours apart with or without food. ( 2.1 ) • INLYTA should be swallowed whole with a glass of water. ( 2.1 ) • See Full Prescribing Information for dosage modifications for adverse reactions. ( 2.2 ) • If a strong CYP3A4/5 inhibitor is required, decrease the INLYTA dose by approximately half. ( 2.2 ) • For patients with moderate hepatic impairment, decrease the starting dose by approximately half. ( 2.2 ) 2.1 Recommended Dosing First-Line Advanced RCC INLYTA in Combination with Avelumab The recommended starting dosage of INLYTA is 5 mg orally taken twice daily (12 hours apart) with or without food in combination with avelumab 800 mg administered as an intravenous infusion over 60 minutes every 2 weeks until disease progression or unacceptable toxicity. When INLYTA is used in combination with avelumab, dose escalation of INLYTA above the initial 5 mg dose may be considered at intervals of two weeks or longer. Review the Full Prescribing Information for recommended avelumab dosing information.

Warnings & precautions

Sourced from openFDA

• Hypertension: Hypertension including hypertensive crisis has been observed. Blood pressure should be well-controlled prior to initiating INLYTA. Monitor for hypertension and treat as needed. Withhold and then dose reduce INLYTA or permanently discontinue based on severity of hypertension. ( 5.1 ) • Arterial and Venous Thromboembolic Events: 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. Permanently discontinue INLYTA if an arterial thromboembolic event occurs during treatment. Withhold INLYTA and then resume at same dose or permanently discontinue based on severity of VTE. ( 5.2 , 5.3 ) • Hemorrhage: 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. Withhold and then dose reduce INLYTA or discontinue based on severity and persistence of hemorrhage. ( 5.4 ) • Cardiac Failure: Cardiac failure has been observed and can be fatal. Monitor for signs or symptoms of cardiac failure throughout treatment with INLYTA. Management of cardiac failure may require dose reduction, dose interruption or permanent discontinuation of INLYTA. ( 5.5 ) • Gastrointestinal Perforation and Fistula Formation: Gastrointestinal perforation and fistula, including death, have occurred. Use with caution in patients at risk for gastrointestinal perforation or fistula.

Adverse reactions

Sourced from openFDA

The following clinically significant adverse reactions are discussed elsewhere in the labeling [see Warnings and Precautions (5) ] : • Hypertension [see Warnings and Precautions (5.1) ] • Arterial thromboembolic events [see Warnings and Precautions (5.2) ] • Venous thromboembolic events [see Warnings and Precautions (5.3) ] • Hemorrhage [see Warnings and Precautions (5.4) ] • Cardiac failure [see Warnings and Precautions (5.5) ] • Gastrointestinal perforation and fistula formation [see Warnings and Precautions (5.6) ] • Thyroid dysfunction [see Warnings and Precautions (5.7) ] • Reversible posterior leukoencephalopathy syndrome [see Warnings and Precautions (5.9) ] • Proteinuria [see Warnings and Precautions (5.10) ] • Hepatotoxicity [see Warnings and Precautions (5.11) ] • Hepatic impairment [see Warnings and Precautions (5.12) ] Most common adverse reactions (≥20%) are: INLYTA in combination with avelumab: diarrhea, fatigue, hypertension, musculoskeletal pain, nausea, mucositis, palmar-plantar erythrodysesthesia, dysphonia, decreased appetite, hypothyroidism, rash, hepatotoxicity, cough, dyspnea, abdominal pain, and headache. ( 6.1 ) INLYTA in combination with pembrolizumab: diarrhea, fatigue/asthenia, hypertension, hepatotoxicity, hypothyroidism, decreased appetite, palmar-plantar erythrodysesthesia, nausea, stomatitis/mucosal inflammation, dysphonia, rash, cough, and constipation.

Use in specific populations

Sourced from openFDA

Lactation: Advise not to breastfeed. ( 8.2 ) 8.1 Pregnancy Risk Summary Based on findings in animal studies and its mechanism of action, INLYTA can cause fetal harm when administered to a pregnant woman. There are no available human data to inform the drug-associated risk. In developmental toxicity studies, axitinib was teratogenic, embryotoxic and fetotoxic in mice at exposures lower than human exposures at the recommended starting dose (see Data ) . Advise females of reproductive potential of the potential risk to a fetus. The background risk of major birth defects and miscarriage for the indicated populations are unknown. However, the background risk in the United States (U.S.) general population of major birth defects is 2%–4% and of miscarriage is 15%–20% of clinically recognized pregnancies. When INLYTA is used in combination with avelumab or pembrolizumab, refer to the full prescribing information of avelumab or pembrolizumab for pregnancy information. Data Animal Data Oral axitinib administered twice daily to female mice prior to mating and through the first week of pregnancy caused an increase in post-implantation loss at all doses tested (≥15 mg/kg/dose, approximately 10 times the systemic exposure (AUC) in patients at the recommended starting dose).

Pharmacokinetics

Sourced from openFDA
Metabolism
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.

Overdosage

Sourced from openFDA

There is no specific treatment for INLYTA overdose. In a controlled clinical study with INLYTA for the treatment of patients with RCC, 1 patient inadvertently received a dose of 20 mg twice daily for 4 days and experienced dizziness (Grade 1). In a clinical dose finding study with INLYTA, subjects who received starting doses of 10 mg twice daily or 20 mg twice daily experienced adverse reactions which included hypertension, seizures associated with hypertension, and fatal hemoptysis. In cases of suspected overdose, INLYTA should be withheld and supportive care instituted.

Approval history

Sourced from openFDA
  • Jan 27, 2012NDANDA202324Pf Prism Cv

FAERS reports

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Reference statistics only. FAERS reports are voluntarily submitted and are not incidence rates, safety signals, or causal evidence. Counts reflect reporting volume — how often a reaction was reported, not how often it occurs. For decision-grade use, consult openFDA and the FAERS Public Dashboard directly.
19,195 total reports matchedLatest report Share = reports listing the reaction ÷ total matched reports. Rows can sum to >100% because a single report often lists multiple reactions.
  1. 1Death2,63514%
  2. 2Diarrhoea2,56513%
  3. 3Fatigue2,10611%
  4. 4Neoplasm Progression1,3236.9%
  5. 5Hypertension1,3216.9%
  6. 6Disease Progression1,2116.3%
  7. 7Off Label Use1,2006.3%
  8. 8Nausea1,1425.9%
  9. 9Decreased Appetite1,0835.6%
  10. 10Dysphonia1,0095.3%
  11. 11Blood Pressure Increased8484.4%
  12. 12Weight Decreased7984.2%
  13. 13Asthenia7583.9%
  14. 14Headache6043.1%
  15. 15Stomatitis5913.1%

Literature

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Recent PubMed references pinned to Axitinib as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.

Clinical trials

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The 10 most recently updated of 236 ClinicalTrials.gov registrations naming Axitinib as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

Frequently asked questions

How does Axitinib work?
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.
What is Axitinib used for?
According to FDA labeling, Axitinib carries indications including: INLYTA is a kinase inhibitor indicated: • in combination with avelumab, for the first-line treatment of patients with advanced renal cell carcinoma (RCC). ( 1.1 ) • in combination with pembrolizumab, for the first-line treatment of patients with advanced RCC.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.
What class of drug is Axitinib?
Axitinib is classified as Vascular endothelial growth factor receptor (VEGFR) tyrosine kinase inhibitors, Kinase Inhibitor, Receptor Tyrosine Kinase Inhibitors, Cellular Proliferation Alteration.
What are the brand names for Axitinib?
Axitinib is marketed under brand names including Inlyta.
What are the contraindications for Axitinib?
Axitinib labeling lists contraindications including: None. None.. Always consult the full prescribing information and a clinician.
Note. Data for axitinib is illustrative MVP content compiled from public sources. pharmacopeia is for educational and informational use only and is not a substitute for professional medical advice.

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