Axitinib (Oral)

Axitinib, also known by its brand name of Inlyta, is a small molecule tyrosine kinase inhibitor approved for the treatment of renal cell carcinoma

Overview

What is Axitinib?

Axitinib is a receptor protein-kinase inhibitor drug that acts to inhibit the vascular growth factor actions and also inhibits angiogenesis. Axitinib is prescribed in a pill format to be swallowed whole with water and taken with or without food. Dosage varies depending on general health, type of cancer or condition and other factors specific to each patient.

How does Axitinib work?

Axitinib is considered a targeted therapy drug, which is the result of almost 100 years of research to understand how cancer cells and normal cells work. Instead of targeting the common trait that cancer cells of rapid division, which leads to side effects in other cells that have this trait, targeted therapy identifies other features of cancer cells and targets those. Some targeted therapies focus on the internal components and function of the cell; others target receptors on the outside of the cell and others starve the cell by targeting the blood vessels that supply the cells.

Axitinib targets and binds to the vascular endothelial growth factor receptors that are found on the inside of cancer cells. By binding to these receptors, Axitinib blocks a vital pathway that promotes blood vessel creation by the cell. This eventually kills the cancer cell, but it does cause certain side effects.

What cancers is Axitinib most effective on?

Axitinib is most commonly prescribed for patients who have advanced renal cell carcinoma and have already been through at least one failed treatment.

What is renal cell carcinoma?

Renal cell carcinoma originates in the lining of the proximal convoluted tubule, part of the tiny tubes found in the kidneys that do the work of transporting urine. Renal cell carcinoma represents 90 to 95% of the cases of kidney cancer diagnosed in adults.

People with renal cell carcinoma often don't have symptoms, so the disease may be in an advanced stage by the time it's discovered. Symptoms include:

  • Blood in the urine
  • Pain in the side, abdomen or flank,
  • Weight loss
  • Fever
  • Hypertension
  • Night sweats
  • Generally unwell feeling

Partial or complete removal is the most common initial treatment if the cancer has not metastasized, which offers a good survival rate. Targeted therapy drugs such as Axitinib give new hope by improving the outlook for metastatic renal cell carcinoma.

Conditions treated

  • Renal cell carcinoma

Type of Medicine

  • Tyrosine kinase antineoplastic agent inhibitor

Side effects

As Axitinib goes about its work of targeting specific traits of the renal cell carcinoma cells to kill them off, it may also cause side effects by the effect it has on normal cells. If you experience any of the side effects listed here, contact your physician immediately.

Common side effects include:

  • Abdominal pain
  • Stomach pain
  • Confusion
  • Constipation
  • Cough with blood
  • Bloody gums
  • Bleeding nose
  • Vision that is blurry
  • Urine that appears cloudy
  • Decreased urine
  • Depression
  • Difficulty breathing
  • Swallowing is difficult
  • Dizziness
  • Mouth, skin or hair is dry
  • Fainting
  • Cold feeling
  • Loss of hair
  • Hoarse voice
  • Incoherence
  • Menstrual flow has increased
  • Increased urine
  • Nausea
  • Nosebleeds
  • Nervousness
  • Paralysis
  • Rapid breathing
  • Ear pounding
  • Stools appear red or tar like
  • Urine is dark brown or red
  • Lightheadedness
  • Loss of appetite
  • Metallic taste
  • Muscle cramps
  • Stiff muscles
  • Muscle weakness
  • Red, swollen, painful skin
  • Scaly skin on feet or hands
  • Heartbeat is rapid or sluggish
  • Eyes are sunken
  • Thirsty
  • Tightness in the chest
  • Feet and hands tingle
  • Skin ulcers
  • Unusual fatigue
  • Vomiting
  • Weight fluctuation
  • Wrinkles

Less common side effects include:

  • Anxiety
  • Bleeding nose or gums
  • Extreme drowsiness
  • Eye pain
  • Heartburn
  • Inability to speak
  • Bleeding rectum
  • Stools are bloody or tar-like
  • Vision changes
  • Chest pain
  • Indigestion
  • Numbness in legs, hands, arms or face
  • Leg or chest pain
  • Pain in arms, jaw, neck, back
  • Painful, red, swollen leg or arm
  • Paleness
  • Ringing ears
  • Seizures
  • Heat sensitivity
  • Sudden, severe headaches
  • Severe stomach cramping or pain
  • Slurred speech
  • Coordination is lost
  • Trouble with breathing
  • Changes in vision
  • Sweating
  • Blindness that is temporary
  • Insomnia
  • Trouble walking, thinking, speaking
  • Breathing is troubled or labored
  • Swelling around anus
  • Bleeding or bruising that is unusual or unexpected
  • Vomiting coffee ground-like material
  • Weakness on one side in leg or arm

Occasionally side effects occur that aren't severe or potentially dangerous. These unwanted effects typically lessen as treatment with Axitinib continues after the body adjusts to the drug. Your physician can assist you with ways to lessen or eliminate side effects. Contact your physician and let them know should the side effects worsen or become prolonged.

Common side effects:

  • Belching
  • Taste changes
  • Coughing
  • Lips are cracked
  • No appetite
  • Diarrhea
  • Moving is difficult
  • Rash or skin that itches
  • Pain in joints
  • Weakness
  • No taste sensation
  • Pain or aches in muscles
  • Leg or arm pains
  • Throat is sore
  • Pain in the upper stomach
  • White spots, ulcers or sores on the tongue, inside the mouth or on the lips
  • Upset stomach or stomach discomfort
  • Swollen mouth
  • Joins that are swollen
  • Changes in voice

Less common side effects include:

  • Tongue feels like its burning
  • Noises that are unexplained like ringing or buzzing
  • Skin flushes or turns red
  • Loss of hearing
  • Hair is getting thin
  • Skin feels warm

Dosage

Axitinib should be taken only as your doctor has prescribed, even if you aren't feeling well. Do not increase the dose or frequency or prolong the use of this medication. To do so is to risk unwanted side effects that may cause severe health issues.

All provided patient information included with your prescription packaging should be read and understood. Any questions you have should be directed to your doctor or pharmacist.

Take Axitinib with or without food, swallowing the entire tablet with a full glass of water. Do not cut, chew or crush the tablet. Avoid eating grapefruit or drinking grapefruit juice, which could change the way your body absorbs Axitinib.

Different patients have different symptoms and severity of their conditions, so the dosage of this medication has been specifically determined for you by your doctor for your specific health situation. The following is representative of an average dose of Axitinib; your dose may vary.

Adults will typically be prescribed five milligrams to be taken twice per day, at least 12 hours apart. This dose may be adjusted as needed and tolerated by the patient. Children who are prescribed Axitinib have had their dosage determined by their doctor for their specific health condition.

Missing a dose does not mean you should catch up, if you are close to the time of the next dose, do not take the missing dose and resume your medication schedule without double dosing. If you vomit after taking Axitinib, contact your health care professional for instructions on what to do about that dose.

Major Drug Interactions

If you've had an allergic or unusual reaction to Axitinib or other medications, inform your doctor before beginning treatment with this drug. Allergies to animals, foods, dyes or preservatives should also be disclosed to your health care provider.

Studies in pediatric and geriatric age groups have not shown any age-related side effects that were more of a risk with regard to the use of this drug. Prescription of Axitinib to these patients will be at the doctor's discretion.

Pregnant women, or women who may become pregnant, should not be prescribed Axitinib as it has demonstrated fetal risks. Options of therapy should be discussed with your physician.

No studies with adequate data have been done on breastfeeding women to determine if Axitinib passes risks on to breastfeeding infants. Discuss this treatment with your health care provider if you're breastfeeding.

It is of critical importance that you disclose your full medical history as well as details of any drugs you are currently taking or have taken in the recent past before you begin to use Axitinib or any other drug. Be certain to include all prescription as well as non-prescription medications you may be taking and details of any vitamin, herbal or holistic supplements or treatments you are currently taking or have taken in the recent past.

Prescription doses of Axitinib are not typically recommended for use of the medications in the following list but may be mandatory under certain circumstances. Your physician may choose to change dosage or frequency if you are prescribed one of these medications while taking Axitinib:

  • Atazanavir
  • Boceprevir
  • Bosentan
  • Enzalutamide
  • Etravirine
  • Fosphenytoin
  • Indinavir
  • Nefazodone
  • Nelfinavir
  • Phenobarbital
  • Phenytoin
  • Posaconazole
  • Primidone
  • Itraconazole
  • Ketoconazole
  • Lopinavir
  • Lumacaftor
  • Mitotane
  • Modafinil
  • Nafcillin
  • Rifampin
  • Ritonavir
  • Saquinavir
  • Telaprevir
  • Telithromycin
  • Voriconazole
  • Carbamazepine
  • Clarithromycin
  • Conivaptan
  • Efavirenz

Discuss the use of Axitinib in conjunction with alcoholic beverages, tobacco or illegal drugs with your health care professional in case of interactions. Do not take Axitinib with grapefruit or grapefruit juice.

These medical problems are known to affect the effectiveness and/or increase the risks associated with the treatment of Axitinib. Make sure your doctor is aware of any conditions you have prior to treatment with this drug. These conditions include:

  • Stomach or bowel fistula (a hole or opening)
  • Blood that doesn't clot
  • Deep vein thrombosis (blood clot in the leg)
  • Bleeding problems
  • Heart failure
  • Hypertensive symptoms
  • Heart attack
  • Pulmonary embolism (blood clot in the lung)
  • Retinal artery or vein occlusion (blood clot in the eye)

Use of Axitinib with the following medical conditions may worsen their symptoms or make the condition itself worse:

  • Transient ischemic attack
  • Thyroid problems
  • Liver disease

Warnings

Prolonged use of Axitinib requires regular office visits to your health care provider to check for any undesired side effects through urine and/or blood testing. Check and log blood pressure readings regularly when on this medication to make sure it is not too high. If you are experiencing hypertension symptoms you may have the following: dizziness, nervousness, pounding noises, headache, or irregular heartbeat.

Axitinib has been known to cause serious heart and blood vessel problems for some who take it. Notify your physician immediately if you experience discomfort or pain in the chest, one area of your body is weak or numb, discomfort in your jaw, back, arms or neck or shortness of breath, trouble when speaking or changes in your vision.

Do not use Axitinib while pregnant as it can harm unborn children. This medication has been shown to be a cause of birth defects when used by the father if his partner should become pregnant. Using effective birth control is advised while being treated with Axitinib for both men and women. If it is possible that you are pregnant or your partner has become so while using Axitinib, inform your health care provider immediately.

Notify your health care professional right away if you witness any rapid gaining of weight, shortness of breath, chest discomfort or pain, extreme fatigue, weakness, irregular breathing or heartbeat or excessive hand, wrist, feet or ankle swelling, as these could be signs of water retention or heart problems.

If you experience severe burning in the stomach, pains or cramp, bloody stools that appear tarry or black, breathing issues, heartburn, nausea, indigestion, or vomiting coffee ground-like material you may have developed a bowel issue of a serious nature; contact your healthcare provider right away.

Axitinib may give you greater chances of bleeding or cause delays in the healing process of in any wounds you may sustain. For this reason, do not engage in contact sports or activities where you risk injury, bruising or cuts. Dental hygiene such as brushing and flossing should be done with care; explore other options of dental hygiene while on Axitinib. Take care when using objects that have a sharp edge like razors, kitchen utensils or other implements.

Any doctor or dentist who provides you with care needs to be aware that you're on a course of treatment with Axitinib so that they can take proper precautions. A pause in this medication may be necessary at least 24 hours before any surgery you may need to undergo.

A condition formed in the brain named RPLS is an increased risk in patients who are being treated with Axitinib. Symptoms include seizures, headaches, extreme drowsiness, vision problems or confusion. Contact your healthcare professional immediately if you experience any of these symptoms.

Hand-foot syndrome, which is a serious skin problem, may also be at a higher risk for patients on Axitinib. Symptoms of this syndrome include skin rashes or redness, painful swelling or blistered skin on the soles of your feet or palms of your hands and should be reported to your physician right away.

Do not combine this medicine with any others unless specifically prescribed by your physician, including any and all prescription and non-prescription medications as well as vitamin, herbal and holistic therapies you may take.

Storage

This medication should be stored out of sight and reach of children and pets in the original container, kept closed for safety. Keep Axitinib at room temperature and away from heat, moisture and light. Do not allow this medication to freeze.

Should you have expired Axitinib or doses that you don't use, contact your physician or pharmacist on the safest way to dispose of this medication.

Summary

Axitinib is a cancer drug prescribed by doctors also known as Inlyta, that is a tyrosine kinase antineoplastic agent inhibitor designed to specifically target and kill renal cell carcinoma cancer cells to hopefully cause remission and prolong the life of the patient. Axitinib is available in pill form and should be swallowed whole with a full glass of water, either with or without food.

Axitinib works by binding itself to the vascular endothelial growth factor receptors found on the inside of renal cell carcinoma cells and blocking the pathway they use to make blood vessels. This effectively cuts off the blood supply to the cancer and eventually kills the disease.

Occasionally, side effects are reported with the treatment of Axitinib, which include diarrhea, hypertension, fatigue or loss of appetite, nausea, hoarseness, decreased kidney function and anemia. Severe or prolonged instances of side effects should be reported to your health care provider immediately.

Serious side effects may include bleeding events, perforation of stomach or intestine, blood clots, reversible posterior leukoencephalopathy syndrome or hand and foot syndrome. Special attention should be paid to any symptoms of these conditions and your doctor should be notified immediately. Avoid dangerous situations and extreme sports and practice caution with sharp objects, as Axitinib can cause you to bleed more easily and slow the blood clotting reaction.

Axitinib may react with other drugs, so it is encouraged that you disclose any and all drug therapies including prescription, non-prescription, vitamin or holistic treatments to your physician before beginning a course of treatment with Axitinib. Disclosure of your full medical history is also advised.

Store Axitinib in medication its original closed packaging at room temperature and out of sight and reach of children and pets. Do not expose this medication to heat, light or moisture and keep it from freezing. Dispose of unused or expired Axitinib per your doctor or pharmacist's instructions on safe disposal.

Resources
Last Reviewed:
December 24, 2017
Last Updated:
April 04, 2018