Anagrelide

The precise mechanism by which anagrelide reduces blood platelet count is unknown. In cell culture studies, anagrelide suppressed expression of transcription factors including GATA-1 and FOG-1 required for megakaryocytopoiesis, ultimately leading to reduced platelet production.

• & USAGE Anagrelide capsules are indicated for the treatment of patients with thrombocythemia, secondary to myeloproliferative neoplasms, to reduce the elevated platelet count and the risk of thrombosis and to ameliorate associated symptoms including thrombo-hemorrhagic events. Anagrelide is a platelet reducing agent indicated for the treatment of thrombocythemia, secondary to myeloproliferative neoplasms, to reduce the elevated platelet count and the risk of thrombosis and to ameliorate associated symptoms including thrombo-hemorrhagic events.

• None.contraindicated

DOSAGE & ADMINISTRATION The starting dose for adults is 0.5 mg four times a day or 1 mg twice a day. (2.1) The starting dose for pediatric patients is 0.5 mg per day. (2.1) Maintain the starting dose for at least one week and then titrate to maintain target platelet counts. (2.2) Do not exceed a dose increment of 0.5 mg/day in any one week. Do not exceed 10 mg/day or 2.5 mg in a single dose. (2.2) Moderate hepatic impairment: Start with 0.5 mg per day. (2.3) 2.1 Recommended Starting Dosage Adults: The recommended starting dosage of anagrelide capsules is 0.5 mg four times daily or 1 mg twice daily. Pediatric Patients: The recommended starting dosage of anagrelide capsules is 0.5 mg daily. 2.2 Dose Titration Based Upon Platelet Response Continue the starting dose for at least one week and then titrate to reduce and maintain the platelet count below 600,000/μL, and ideally between 150,000/μL and 400,000/μL. The dose increment should not exceed 0.5 mg/day in any one week. Dosage should not exceed 10 mg/day or 2.5 mg in a single dose. Most patients will experience an adequate response at a dose of 1.5 to 3.0 mg/day. Monitor platelet counts weekly during titration then monthly or as necessary. 2.3 Dose Modifications for Hepatic Impairment In patients with moderate hepatic impairment (Child Pugh score 7-9) start anagrelide capsules therapy at a dose of 0.5 mg/day and monitor frequently for cardiovascular events [see Warnings and Precautions (5.1), Use in Specific Populations (8.6) and Clinical Pharmacology (12.3)] .

Cardiovascular Toxicity: QT prolongation and ventricular tachycardia have been reported with anagrelide. Obtain a pre-treatment cardiovascular examination including an ECG in all patients. Monitor patients for cardiovascular effects. (5.1) Pulmonary Hypertension: Assess underlying cardiopulmonary disease prior to initiating therapy. (5.2) Bleeding Risk: Monitor patients for bleeding, including those receiving concomitant therapy with other drugs known to cause bleeding. (5.3) 5.1 Cardiovascular Toxicity Torsades de pointes and ventricular tachycardia have been reported with anagrelide. Obtain a pre-treatment cardiovascular examination including an ECG in all patients. During treatment with anagrelide monitor patients for cardiovascular effects and evaluate as necessary. Anagrelide increases the QTc interval of the electrocardiogram and increases the heart rate in healthy volunteers [see Clinical Pharmacology (12.2)] . Do not use anagrelide in patients with known risk factors for QT interval prolongation, such as congenital long QT syndrome, a known history of acquired QTc prolongation, medicinal products that can prolong QTc interval and hypokalemia [see Drug Interactions (7.1)] . Hepatic impairment increases anagrelide exposure and could increase the risk of QTc prolongation. Monitor patients with hepatic impairment for QTc prolongation and other cardiovascular adverse reactions. The potential risks and benefits of anagrelide therapy in a patient with mild and moderate hepatic impairment should be assessed before treatment is commenced.

The following clinically significant adverse reactions are discussed in greater detail in other sections of the labeling: Cardiovascular Toxicity [see Warnings and Precautions (5.1)] Pulmonary Hypertension [see Warnings and Precautions (5.2)] Bleeding Risk [see Warnings and Precautions (5.3)] Pulmonary Toxicity [see Warnings and Precautions (5.4)] The most common adverse reactions (incidence ≥ 5%) are headache, palpitations, diarrhea, asthenia, edema, nausea, abdominal pain, dizziness, pain, dyspnea, cough, flatulence, vomiting, fever, peripheral edema, rash, chest pain, anorexia, tachycardia, malaise, paresthesia, back pain, pruritus, and dyspepsia. (6.1) To report SUSPECTED ADVERSE REACTIONS, contact ANI Pharmaceuticals, Inc. at 1-855-204-1431 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. Clinical Studies in Adult Patients In three single-arm clinical studies, 942 patients [see Clinical Trials (14)] diagnosed with myeloproliferative neoplasms of varying etiology (ET: 551; PV: 117; OMPN: 274) were exposed to anagrelide with a mean duration of approximately 65 weeks.

Lactation: Advise not to breastfeed. (8.2) 8.1 Pregnancy Risk Summary Available data from case reports with anagrelide use in pregnant women have not identified a drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes. In animal embryo-fetal studies, delayed fetal development (delayed skeletal ossification and reduced body weight) was observed in rats administered anagrelide hydrochloride during organogenesis at doses approximately 97 times the maximum clinical dose (10 mg/day) based on body surface area (see Data) . There are adverse effects on maternal and fetal outcomes associated with thrombocythemia in pregnancy (see Clinical Considerations). The estimated background risk of major birth defects and miscarriage for the indicated population is unknown. All pregnancies have a background risk of birth defect, loss, or other adverse outcomes. In the U.S. general population, the estimated background risk of major birth defect and miscarriage in clinically recognized pregnancies is 2% to 4% and 15% to 20%, respectively. Clinical Considerations Disease-Associated Maternal and/or Embryo/Fetal Risk Thrombotic events, such as stroke, deep vein thrombosis, or myocardial infarction, can be complications of thrombocythemia.

Metabolism

Dose proportionality has been found in the dose range 0.5 mg to 2.5 mg. Absorption Following oral administration of anagrelide, at least 70% is absorbed from the gastrointestinal tract.

At higher than recommended doses, anagrelide has been shown to cause hypotension. There have been postmarketing case reports of intentional overdose with anagrelide. Reported symptoms include sinus tachycardia and vomiting. Symptoms resolved with supportive management. Platelet reduction from anagrelide therapy is dose-related; therefore, thrombocytopenia, which can potentially cause bleeding, is expected from overdosage. In case of overdosage, stop anagrelide dosing and monitor platelet counts for thrombocytopenia and observe for possible complications such as bleeding. Consider resumption of anagrelide dosing once the platelet count returns to the normal range.

• Mar 14, 1997NDANDA020333Takeda Pharms Usa
• Apr 18, 2005ANDAANDA076683Chartwell Rx
• Apr 18, 2005ANDAANDA076811Novitium Pharma
• Jun 30, 2017ANDAANDA209151Torrent

1. 1Off Label Use2079.2%
2. 2Platelet Count Increased1556.9%
3. 3Fatigue1476.5%
4. 4Headache1295.7%
5. 5Anaemia1255.6%
6. 6Haemoglobin Decreased1064.7%
7. 7Diarrhoea1054.7%
8. 8Dizziness954.2%
9. 9Drug Ineffective954.2%
10. 10Dyspnoea924.1%
11. 11Death853.8%
12. 12Nausea813.6%
13. 13Asthenia793.5%
14. 14Myelofibrosis703.1%
15. 15Fall622.8%

The 10 most recently updated of 29 ClinicalTrials.gov registrations naming Anagrelide as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• A Study of Bomedemstat (IMG-7289/MK-3543) Compared to Best Available Therapy (BAT) in Participants With Essential Thrombocythemia and an Inadequate Response or Intolerance of Hydroxyurea (MK-3543-006)
  Recruiting · Phase 3 · Interventional · 340 enrolled · Merck Sharp & Dohme LLC
  NCT06079879updated 2026-06-12
• A Study to Evaluate Single Agent Selinexor Versus Physician's Choice in Participants With Previously Treated Myelofibrosis
  Active not recruiting · Phase 2 · Interventional · 112 enrolled · Karyopharm Therapeutics Inc
  NCT04562870updated 2025-10-03
• Ropeginterferon Alfa-2b (P1101) vs. Anagrelide in Essential Thrombocythemia Patients With Hydroxyurea Resistance or Intolerance
  Active not recruiting · Phase 3 · Interventional · 174 enrolled · PharmaEssentia
  NCT04285086updated 2025-08-13
• The Ruxo-BEAT Trial in Patients With High-risk Polycythemia Vera or High-risk Essential Thrombocythemia
  Active not recruiting · Phase 2 · Interventional · 207 enrolled · RWTH Aachen University
  NCT02577926updated 2025-06-10
• Fasting Study of Anagrelide Hydrochloride Capsules 1 mg to Agrylin® Capsules 1 mg
  Completed · Phase 1 · Interventional · 47 enrolled · Mylan Pharmaceuticals Inc
  NCT00648024updated 2024-04-24
• Fed Study of Anagrelide Hydrochloride Capsules 1 mg to Agrylin® Capsules 1 mg
  Completed · Phase 1 · Interventional · 22 enrolled · Mylan Pharmaceuticals Inc
  NCT00648765updated 2024-04-24
• Efficacy of Momelotinib Versus Best Available Therapy in Anemic or Thrombocytopenic Subjects With Primary Myelofibrosis (MF), Post-polycythemia Vera MF, or Post-essential Thrombocythemia MF
  Completed · Phase 3 · Interventional · 156 enrolled · Sierra Oncology LLC - a GSK company
  NCT02101268updated 2023-05-23
• Agrylin Drug Use-Result Survey
  Completed · Observational · 1,826 enrolled · Takeda
  NCT03625895updated 2023-02-27
• Nilotinib as First-line Treatment of Ph+ CML in Early Chronic Phase
  Completed · Phase 2 · Interventional · 74 enrolled · Gruppo Italiano Malattie EMatologiche dell'Adulto
  NCT00481052updated 2022-01-18
• Phase 2 Study of Ruxolitinib Versus Anagrelide in Subjects With Essential Thrombocythemia Who Are Resistant to or Intolerant of Hydroxyurea (RESET-272)
  Terminated · Phase 2 · Interventional · 12 enrolled · Incyte Corporation
  NCT03123588updated 2021-11-19

Frequently asked questions

How does Anagrelide work?

The precise mechanism by which anagrelide reduces blood platelet count is unknown. In cell culture studies, anagrelide suppressed expression of transcription factors including GATA-1 and FOG-1 required for megakaryocytopoiesis, ultimately leading to reduced platelet production.

What is Anagrelide used for?

According to FDA labeling, Anagrelide carries indications including: & USAGE Anagrelide capsules are indicated for the treatment of patients with thrombocythemia, secondary to myeloproliferative neoplasms, to reduce the elevated platelet count and the risk of thrombosis and to ameliorate associated symptoms including thrombo-hemorrhagic events. Anagrelide is a platelet reducing agent indicated for the treatment of thrombocythemia, secondary to myeloproliferative neoplasms, to reduce the elevated platelet count and the risk of thrombosis and to ameliorate associated symptoms including thrombo-hemorrhagic events.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Anagrelide?

Anagrelide is classified as Other antineoplastic agents, Platelet-reducing Agent, Phosphodiesterase 3 Inhibitors, Phosphodiesterase Inhibitors, Decreased Platelet Production.

What are the brand names for Anagrelide?

Anagrelide is marketed under brand names including Agrylin.

What are the contraindications for Anagrelide?

Anagrelide labeling lists contraindications including: None.. Always consult the full prescribing information and a clinician.