Anagrelide
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Also known as AnagrelidaSID26755034SID124892336ANAGRELIDE HYDROCHLORIDEAnagrelid
Summary
Anagrelide (CHEMBL760) is an approved small-molecule anticoagulant (ATC L01XX35) targeting PDE3A; indicated across 4 conditions including neoplasm and essential thrombocythemia.
At a glance
- Status: Approved (max clinical phase 4)
- Modality: Small molecule
- ATC class: L01XX35
- Targets: 1 (PDE3A)
- Indications: 4 conditions
- Clinical trials: 14
- Chemistry: 256.08 Da · C10H7Cl2N3O
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL760 |
| Name | Anagrelide |
| Type | Small molecule |
| Max phase | 4 |
| FDA approved | yes |
| PubChem CID | 135409400 |
| ChEBI | CHEBI:142290 |
| ATC | L01XX35 |
| Molecular formula | C10H7Cl2N3O |
| Molecular weight | 256.08 |
| InChIKey | OTBXOEAOVRKTNQ-UHFFFAOYSA-N |
SMILES: C1C2=C(C=CC(=C2Cl)Cl)N=C3N1CC(=O)N3
IUPAC name: 6,7-dichloro-3,5-dihydro-1H-imidazo[2,1-b]quinazolin-2-one
ChEBI definition: A 1,5-dihydroimidazo[2,1-]quinazoline having an oxo substituent at the 2-position and chloro substituents at the 6- and 7-positions.
Pharmacological roles (ChEBI): anticoagulant, platelet aggregation inhibitor, antifibrinolytic drug, cardiovascular drug.
Also known as: Anagrelida, Anagrelide, SID26755034, anagrelide, ANAGRELIDE, SID124892336, ANAGRELIDE HYDROCHLORIDE, Anagrelid
Parent form; salt/anhydrous children: CHEMBL1200759
Patent coverage: 5,457 distinct patent families (23,754 SureChEMBL compound mentions), from 3 matched compound structure(s). One matched structure accounts for 22,312 (94%) of the total. Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.
Targets
Targets
Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).
| Gene | Target | Action | pAffinity | Cancer dependency | UniProt |
|---|---|---|---|---|---|
| PDE3A | phosphodiesterase 3A | Inhibition | 7.27 | 0.1% | Q14432 |
Broader ChEMBL bioactivity targets: 5 (assay-derived). Sample: P2Y purinoceptor 12, Menin/Histone-lysine N-methyltransferase MLL, Phosphodiesterase 3, cGMP-inhibited 3’,5’-cyclic phosphodiesterase 3A, cGMP-dependent 3’,5’-cyclic phosphodiesterase.
Bioactivity
ChEMBL activities: 10 potent at pChembl ≥ 5 of 13 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| PDE3B | 9.05 | IC50 | 0.9 | nM | CHEMBL_ACT_25084349 |
| PDE3B | 7.52 | IC50 | 30 | nM | CHEMBL_ACT_25084345 |
| PDE3A | 7.31 | AC50 | 48.9 | nM | CHEMBL_ACT_25190850 |
| PDE3B | 7.3 | IC50 | 50 | nM | CHEMBL_ACT_791075 |
| PDE3B | 7.27 | IC50 | 54 | nM | CHEMBL_ACT_1135378 |
| PDE3B | 7.1 | IC50 | 80 | nM | CHEMBL_ACT_283490 |
| PDE3B | 7.1 | IC50 | 80 | nM | CHEMBL_ACT_917619 |
| PDE3B | 7.09 | IC50 | 82 | nM | CHEMBL_ACT_1136483 |
| P2RY12 | 5.98 | EC50 | 1050 | nM | CHEMBL_ACT_1135380 |
| PDE3B | 5.98 | IC50 | 1050 | nM | CHEMBL_ACT_1200433 |
Target pathways
Aggregated over 1 target gene(s): PDE3A.
Top Reactome pathways
1 total, by targets touching each:
| Pathway | Targets | Genes |
|---|---|---|
| G alpha (s) signalling events | 1 | PDE3A |
Dominant GO biological processes
| GO term | Targets |
|---|---|
| oocyte maturation | 1 |
| lipid metabolic process | 1 |
| G protein-coupled receptor signaling pathway | 1 |
| response to xenobiotic stimulus | 1 |
| regulation of meiotic nuclear division | 1 |
| negative regulation of apoptotic process | 1 |
| negative regulation of vascular permeability | 1 |
| positive regulation of vascular permeability | 1 |
| positive regulation of oocyte development | 1 |
| regulation of ribonuclease activity | 1 |
| cellular response to cGMP | 1 |
| cellular response to transforming growth factor beta stimulus | 1 |
| apoptotic signaling pathway | 1 |
| negative regulation of adenylate cyclase-activating G protein-coupled receptor signaling pathway | 1 |
| negative regulation of cAMP/PKA signal transduction | 1 |
Indications & clinical
Indications
4 indications (1 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).
| Indication | Trial phase | MONDO | EFO |
|---|---|---|---|
| neoplasm | 4 | MONDO:0005070 | EFO:0000616 |
| essential thrombocythemia | 3 | MONDO:0005029 | EFO:0000479 |
| acquired polycythemia vera | 3 | MONDO:0009891 | EFO:0002429 |
1 further indication record had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.
Clinical trials
Total trials: 14.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE3 | 6 |
| PHASE1 | 3 |
| PHASE2 | 2 |
| PHASE4 | 1 |
| PHASE2/PHASE3 | 1 |
| Not specified | 1 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT00202644 | PHASE4 | COMPLETED | A Study of Anagrelide and Hydroxyurea in High-Risk Essential Thrombocythemia Patients |
| NCT04285086 | PHASE3 | ACTIVE_NOT_RECRUITING | Ropeginterferon Alfa-2b (P1101) vs. Anagrelide in Essential Thrombocythemia Patients With Hydroxyurea Resistance or Intolerance |
| NCT06079879 | PHASE3 | RECRUITING | 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) |
| NCT01065038 | PHASE3 | COMPLETED | Anagrelide vs. Hydroxyurea - Efficacy and Tolerability Study in Patients With Essential Thrombocythaemia |
| NCT01214915 | PHASE3 | COMPLETED | Effect of SPD422 on Platelet Lowering and Safety in Japanese Adults With At Risk Essential Thrombocythaemia |
| NCT01230775 | PHASE3 | COMPLETED | Anagrelide Retard vs. Placebo: Efficacy and Safety in At-risk Patients With Essential Thrombocythaemia |
| NCT02076815 | PHASE3 | COMPLETED | Anagrelide Retard in Essential Thrombocythemia |
| NCT02962388 | PHASE2/PHASE3 | TERMINATED | The Ruxolitinib Versus Best Available Therapy Trial in Patients With High Risk ET in Second Line |
| NCT00413634 | PHASE2 | COMPLETED | The Pharmacokinetics of Anagrelide in Elderly and Young Patients With Essential Thrombocythaemia (ET) |
| NCT03123588 | PHASE2 | TERMINATED | Phase 2 Study of Ruxolitinib Versus Anagrelide in Subjects With Essential Thrombocythemia Who Are Resistant to or Intolerant of Hydroxyurea (RESET-272) |
| NCT00648024 | PHASE1 | COMPLETED | Fasting Study of Anagrelide Hydrochloride Capsules 1 mg to Agrylin® Capsules 1 mg |
| NCT00648765 | PHASE1 | COMPLETED | Fed Study of Anagrelide Hydrochloride Capsules 1 mg to Agrylin® Capsules 1 mg |
| NCT01552928 | PHASE1 | COMPLETED | Effect of Anagrelide Hydrochloride on Any Changes in Heart Function in Healthy Volunteers |
| NCT01352585 | Not specified | COMPLETED | Exploratory Multi-centre Trial In Patients With ET Treated With XAGRID® |
Clinical evidence (CIViC)
No CIViC predictive evidence (expected for non-precision-medicine drugs).
Pharmacology
Pharmacogenomics
No PharmGKB pharmacogenomic data curated for this drug.
Related molecules
Related molecules
Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.
200 molecules share ≥1 primary target. Top 60 by shared-target count:
| Molecule | Source | Status | Shared targets |
|---|---|---|---|
| CLOFARABINE | ChEMBL + PubChem | Phase 4 (approved) | PDE3A |
| IDELALISIB | ChEMBL + PubChem | Phase 4 (approved) | PDE3A |
| LOSARTAN | ChEMBL + PubChem | Phase 4 (approved) | PDE3A |
| TAFAMIDIS | ChEMBL + PubChem | Phase 4 (approved) | PDE3A |
| TAVABOROLE | ChEMBL + PubChem | Phase 4 (approved) | PDE3A |
| ACARBOSE | ChEMBL | Phase 4 (approved) | PDE3A |
| ADENOSINE | ChEMBL | Phase 4 (approved) | PDE3A |
| ALECTINIB | ChEMBL | Phase 4 (approved) | PDE3A |
| ALENDRONIC ACID | ChEMBL | Phase 4 (approved) | PDE3A |
| AMINOGLUTETHIMIDE | ChEMBL | Phase 4 (approved) | PDE3A |
| AMLEXANOX | ChEMBL | Phase 4 (approved) | PDE3A |
| ANTAZOLINE | ChEMBL | Phase 4 (approved) | PDE3A |
| ARIPIPRAZOLE | ChEMBL | Phase 4 (approved) | PDE3A |
| BENAZEPRIL | ChEMBL | Phase 4 (approved) | PDE3A |
| BENZBROMARONE | ChEMBL | Phase 4 (approved) | PDE3A |
| BITHIONOL | ChEMBL | Phase 4 (approved) | PDE3A |
| CABOZANTINIB | ChEMBL | Phase 4 (approved) | PDE3A |
| CALCITRIOL | ChEMBL | Phase 4 (approved) | PDE3A |
| CANDESARTAN CILEXETIL | ChEMBL | Phase 4 (approved) | PDE3A |
| CANNABIDIOL | ChEMBL | Phase 4 (approved) | PDE3A |
| CEFOPERAZONE | ChEMBL | Phase 4 (approved) | PDE3A |
| CHLORHEXIDINE | ChEMBL | Phase 4 (approved) | PDE3A |
| CHLOROQUINE | ChEMBL | Phase 4 (approved) | PDE3A |
| CHOLIC ACID | ChEMBL | Phase 4 (approved) | PDE3A |
| CILOSTAZOL | ChEMBL | Phase 4 (approved) | PDE3A |
| CINNARIZINE | ChEMBL | Phase 4 (approved) | PDE3A |
| CLADRIBINE | ChEMBL | Phase 4 (approved) | PDE3A |
| CODEINE | ChEMBL | Phase 4 (approved) | PDE3A |
| CRISABOROLE | ChEMBL | Phase 4 (approved) | PDE3A |
| DEOXYCHOLIC ACID | ChEMBL | Phase 4 (approved) | PDE3A |
| DEQUALINIUM | ChEMBL | Phase 4 (approved) | PDE3A |
| DIPYRIDAMOLE | ChEMBL | Phase 4 (approved) | PDE3A |
| DISOPYRAMIDE | ChEMBL | Phase 4 (approved) | PDE3A |
| DUVELISIB | ChEMBL | Phase 4 (approved) | PDE3A |
| EFAVIRENZ | ChEMBL | Phase 4 (approved) | PDE3A |
| ENCORAFENIB | ChEMBL | Phase 4 (approved) | PDE3A |
| ENOXIMONE | ChEMBL | Phase 4 (approved) | PDE3A |
| ESTRADIOL CYPIONATE | ChEMBL | Phase 4 (approved) | PDE3A |
| ESTRADIOL VALERATE | ChEMBL | Phase 4 (approved) | PDE3A |
| ETHINYL ESTRADIOL | ChEMBL | Phase 4 (approved) | PDE3A |
| FEXOFENADINE | ChEMBL | Phase 4 (approved) | PDE3A |
| GEMCITABINE | ChEMBL | Phase 4 (approved) | PDE3A |
| GRISEOFULVIN | ChEMBL | Phase 4 (approved) | PDE3A |
| HEXACHLOROPHENE | ChEMBL | Phase 4 (approved) | PDE3A |
| HYDROXOCOBALAMIN | ChEMBL | Phase 4 (approved) | PDE3A |
| HYDROXYPROGESTERONE CAPROATE | ChEMBL | Phase 4 (approved) | PDE3A |
| IBANDRONIC ACID | ChEMBL | Phase 4 (approved) | PDE3A |
| IBUDILAST | ChEMBL | Phase 4 (approved) | PDE3A |
| IDEBENONE | ChEMBL | Phase 4 (approved) | PDE3A |
| IFOSFAMIDE | ChEMBL | Phase 4 (approved) | PDE3A |
| ILOPERIDONE | ChEMBL | Phase 4 (approved) | PDE3A |
| INAMRINONE | ChEMBL | Phase 4 (approved) | PDE3A |
| INDOCYANINE GREEN ACID FORM | ChEMBL | Phase 4 (approved) | PDE3A |
| IRBESARTAN | ChEMBL | Phase 4 (approved) | PDE3A |
| ISOPROTERENOL | ChEMBL | Phase 4 (approved) | PDE3A |
| ISRADIPINE | ChEMBL | Phase 4 (approved) | PDE3A |
| LAMIVUDINE | ChEMBL | Phase 4 (approved) | PDE3A |
| LAMOTRIGINE | ChEMBL | Phase 4 (approved) | PDE3A |
| MASOPROCOL | ChEMBL | Phase 4 (approved) | PDE3A |
| MECLIZINE | ChEMBL | Phase 4 (approved) | PDE3A |
Related Atlas pages
- Genes: PDE3A
- Diseases: neoplasm, essential thrombocythemia, acquired polycythemia vera
- Drugs: Clofarabine, Idelalisib, Losartan, Tafamidis, Tavaborole, Acarbose, Adenosine, Alectinib, Alendronic Acid, Aminoglutethimide, Amlexanox, Antazoline, Aripiprazole, Benazepril, Benzbromarone, Bithionol, Cabozantinib, Calcitriol, Candesartan Cilexetil, Cannabidiol, Cefoperazone, Chlorhexidine, Chloroquine, Cholic Acid, Cilostazol, Cinnarizine, Cladribine, Codeine, Crisaborole, Deoxycholic Acid, Dequalinium, Dipyridamole, Disopyramide, Duvelisib, Efavirenz, Encorafenib, Enoximone, Estradiol Cypionate, Estradiol Valerate, Ethinyl Estradiol, Fexofenadine, Gemcitabine, Griseofulvin, Hexachlorophene, Hydroxocobalamin, Hydroxyprogesterone Caproate, Ibandronic Acid, Ibudilast, Idebenone, Ifosfamide, Iloperidone, Inamrinone, Indocyanine Green Acid Form, Irbesartan, Isoproterenol, Isradipine, Lamivudine, Lamotrigine, Masoprocol, Meclizine