How Do PDGFR-alpha Inhibitors Work?

Reviewed on 11/2/2021

HOW DO PDGFR-ALPHA INHIBITORS WORK?

Platelet-derived growth factor receptor A (PDGFR-A) inhibitors are a class of drugs used to treat gastrointestinal stromal tumors (a type of tumor that grows in the stomach, intestine, bowel, or esophagus [the tube that connects the throat with the stomach]), acute lymphoblastic leukemia (a type of cancer of the blood and bone marrow), chronic myeloid leukemia (a rare type of cancer of the bone marrow), and myelodysplastic/myeloproliferative diseases (a group of diseases in which the bone marrow produces an excess of white blood cells). 

They are also used to treat certain immune system disorders such as aggressive systemic mastocytosis (a rare disorder that results in accumulation of mast cells in the body) and hypereosinophilic syndrome (a group of blood disorders characterized by persistent eosinophilia).

PDGFR-alpha inhibitors are chemotherapy medications and a selective tyrosine kinase inhibitor of KIT and PDGFR-A (a receptor located on the surface of cells) that helps in inhibiting the proliferation of tumor cells and induces apoptosis (death of cells that occurs as a normal and controlled part of an organism's growth or development).

PDGFR-alpha inhibitors are administered via oral route, typically once or twice a day with or without food.

PDGFR-alpha inhibitors work in the following ways:

  • They belong to a class of drugs known as "kinase inhibitors" that work by slowing down or stopping the growth of cancer cells and certain immune system cells (mast cells).
  • They inhibit various gene mutations, increasing progression-free survival in patients with leukemias.

HOW ARE PDGFR-ALPHA INHIBITORS USED?

PDGFR-alpha inhibitors are used to treat conditions such as:

  • Gastrointestinal stromal tumors (a type of tumor located in the gastrointestinal tract)
  • Systemic mastocytosis (a rare disorder that results in the accumulation of mast cells in the body)
  • Acute lymphoblastic leukemia (a type of cancer of the blood and bone marrow)
  • Myelodysplastic/myeloproliferative diseases (a group of diseases in which the bone marrow produces an excess of white blood cells)
  • Hypereosinophilic syndrome (a group of blood disorders characterized by persistent eosinophilia)
  • Chronic eosinophilic leukemia (a rare neoplasm characterized by overproduction of eosinophils in the bone marrow)
  • Chronic Philadelphia chromosome-positive myeloid leukemia (abnormal changes in the chromosomes, leading to high levels of abnormal cells in the bone marrow and blood)
  • Dermatofibrosarcoma protuberans (a tumor that forms under the top layer of the skin

QUESTION

What are risk factors for developing colon cancer? See Answer

WHAT ARE SIDE EFFECTS OF PDGFR-ALPHA INHIBITORS?

Some of the common side effects include:

Other rare side effects include:

Information contained herein is not intended to cover all possible side effects, precautions, warnings, drug interactions, allergic reactions, or adverse effects. Check with your doctor or pharmacist to make sure these drugs do not cause any harm when you take them along with other medicines. Never stop taking your medication and never change your dose or frequency without consulting your doctor.

WHAT ARE NAMES OF PDGFR-ALPHA INHIBITORS?

Generic and brand names of PDGFR-alpha inhibitors include:

References
https://reference.medscape.com/drugs/pdgfr-alpha-inhibitors

https://www.webmd.com/drugs/2/drug-20983/imatinib-oral/details

https://www.webmd.com/drugs/2/drug-179367/ripretinib-oral/details

https://www.webmd.com/drugs/2/drug-178589/avapritinib-oral/details

https://www.fda.gov/drugs/resources-information-approved-drugs/fda-approves-avapritinib-advanced-systemic-mastocytosis

https://medlineplus.gov/druginfo/meds/a620013.html

https://medlineplus.gov/druginfo/meds/a606018.html

https://medlineplus.gov/druginfo/meds/a620035.html

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