Liposomal Tretinoin
Trade Names:
Atragen, Lipo ATRA, Tretinoin Liposomal, AR-623, All-Trans-Retinoic Acid Liposomal
Type of Drug:
Tretinoin is a retinoid used in molecular targeted therapy. A retinoid is a naturally occuring substance in the body that helps to regulate, or control, the work of genes to help cells grow (mature) and divide (reproduce). Liposomal tretinoin is the same drug in a fat molecule. The drug is being studied in patients newly diagnosed with APL, Kaposi's sarcoma, and other types of cancer.
How Drug Works:
Tretinoin causes acute promyelocytic leukemia (APL) cells to mature, thus stopping them from dividing. Giving the drug in a liposome (a fat molecule) allows it to be given intravenously so that the blood levels of the drug may be higher for a longer time than when taken in pill form. This may reduce side effects and overcome resistance that sometimes occurs with the pill form of the drug.
How Drug Is Given:
Liposomal tretinoin is given by an injection in a vein every other day in the beginning of treatment (induction) then 3 times a week for 9 months (maintenance) for promyelocytic leukemia, per clinical trial. It is given 3 times a week for 4 weeks for Kaposi's sarcoma, per clinical trial. The dose depends on your weight, how well you do with the therapy, and certain blood test results (for example, complete blood count, kidney and liver function tests, and cholesterol levels).
Read the following information. If you do not understand it or if any of it causes you special concern, check with your doctor.

Before taking this drug, tell your doctor:

  • If you are trying to become pregnant, are pregnant, or breastfeeding. This drug may cause birth defects if either the male or female is taking it at the time of conception or during pregnancy. Men and women who are taking this drug need to use some kind of birth control. However, do not use oral contraceptives ("the pill") without checking with your doctor.

  • If you think you may want to have children in the future. Many chemotherapy drugs can cause sterility.

  • If you have any of the following medical problems: chickenpox or exposure to chickenpox, gout, heart disease, congestive heart failure, shingles, kidney stones, liver disease, or other forms of cancer.

  • If you are taking any other prescription or over-the-counter drugs, including vitamins and herbals.
Should I avoid any other medicines, foods, alcohol, and/or activities?
Your prescription and nonprescription medicines may interact with other drugs, causing harm. Certain foods or alcohol can also interact with drug products. Never begin taking a new medicine"prescription or nonprescription"without asking your doctor or nurse if it will interact with alcohol, food, or other medicines. Some drug products can cause drowsiness and affect activities such as driving.
Precautions:
Liposomal tretinoin may cause an increase in the following: cholesterol, triglycerides, liver function tests, and kidney function tests. These will all be tested before you begin the drug and monitored during your therapy.
Side effects are less severe than they are with oral tretinoin.
Liposomal tretinoin should not be used by women who are pregnant or breastfeeding, or by patients who are allergic to tretinoin or to any of the liposome components.
Although not common, liposomal tretinoin can cause a syndrome of symptoms. This is called retinoic acid-acute promyelocytic leukemic (RA-APL) syndrome, similar to what can occur with the oral form of tretinoin. You will be watched for and should report fever, difficulty breathing, or joint pain as soon as possible.
Vitamin A toxicity may occur but is less severe than it is with oral tretinoin. This includes headache usually starting the first week of therapy and then fading, fever, dryness of the mouth and skin, bone pain, nausea, vomiting, rash, sores in the mouth, hair loss, and changes in vision. Report any of these to your doctor or nurse right away. Tell your doctor if you are taking any vitamin A products.
Tell all the doctors, dentists, and pharmacists you visit that you are taking this drug.
  • Most of the following side effects probably will not occur.
  • Your doctor or nurse will want to discuss specific care instructions with you.
  • They can help you understand these side effects and help you deal with them.
Side Effects:
More Common Side Effects
  • Headache
  • Fever
  • Dryness of skin and mucous membranes
  • Bone pain
  • Nausea
  • Vomiting
  • Rash
  • Itching
  • Sweating
  • Changes in vision
Less Common Side Effects
  • Difficulty breathing, fever, joint pain (retinoic acid-APL syndrome)
  • Dizziness
  • Difficulty sleeping
  • Confusion
  • Depression
  • Leg weakness
  • Slow speech
  • Facial numbness
  • Forgetfulness
Rare Side Effects
  • Irregular heartbeat
  • Flushing of face
  • Decreased or increased blood pressure
  • Inflammation of veins (phlebitis)
  • Heart failure
  • Bleeding in the gastrointestinal tract
  • Abdominal pain
  • Diarrhea
  • Constipation
  • Heartburn
  • Abdominal swelling
  • Inflammation of the liver (hepatitis)
  • Ulcer
  • Earache
  • Hearing loss
  • Changes in kidney function
  • Enlarged prostate
Side Effects / Symptoms of the Drug

Call your doctor or nurse right away if you have irregular heartbeats, difficulty breathing, blood in your stools, fever, or joint pain.
Other side effects not listed above can also occur in some patients. Tell your doctor or nurse if you develop any problems.
FDA Approval: This drug is being studied for cancer treatment.