anagrelide 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
platelet aggregation inhibitors	209	68475-42-3

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: anagrelide xagrid anagrelide hydrochloride anagrelide hydrochloride hydrate anagrelide HCl anagrelide hydrochloride monohydrate	imidazoquinazoline derivative which lowers platelet count probably by inhibiting thrombopoiesis and reduces platelet aggregation; used for thrombocythemia Molecular weight: 256.09 Formula: C10H7Cl2N3O CLOGP: 1.02 LIPINSKI: 0 HAC: 4 HDO: 1 TPSA: 44.70 ALOGS: -2.96 ROTB: 0 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

anagrelide
xagrid
anagrelide hydrochloride
anagrelide hydrochloride hydrate
anagrelide HCl
anagrelide hydrochloride monohydrate

imidazoquinazoline derivative which lowers platelet count probably by inhibiting thrombopoiesis and reduces platelet aggregation; used for thrombocythemia

Molecular weight: 256.09
Formula: C10H7Cl2N3O
CLOGP: 1.02
LIPINSKI: 0
HAC: 4
HDO: 1
TPSA: 44.70
ALOGS: -2.96
ROTB: 0

Status: OFP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

None

ADMET properties:

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Property	Value	Reference
BA (Bioavailability)	75 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Bocci G, Oprea TI, Benet LZ
MRTD (Maximum Recommended Therapeutic Daily Dose)	0.56 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD

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Approvals:

Date	Agency	Company	Orphan
March 14, 1997	FDA	SHIRE LLC
Nov. 15, 2004	EMA	SHIRE PHARMACEUTICALS IRELAND LIMITED

FDA Adverse Event Reporting System (Female)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Platelet count increased	106.69	31.48	31	1309	17680	63470002
Myelofibrosis	97.87	31.48	18	1322	1359	63486323
Bone marrow reticulin fibrosis	44.22	31.48	7	1333	214	63487468
Thrombocytosis	38.61	31.48	11	1329	5807	63481875
Adenocarcinoma metastatic	33.48	31.48	5	1335	103	63487579

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FDA Adverse Event Reporting System (Male)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Platelet count increased	52.89	27.70	17	1031	9509	34946374
Myelofibrosis	32.96	27.70	8	1040	1603	34954280

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FDA Adverse Event Reporting System (Geriatric)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Platelet count increased	112.32	26.87	36	2098	22370	79719884
Myelofibrosis	66.31	26.87	15	2119	2485	79739769
Thrombocytosis	52.29	26.87	16	2118	8510	79733744
Splenomegaly	38.38	26.87	16	2118	20738	79721516
Bone marrow reticulin fibrosis	32.79	26.87	6	2128	344	79741910
Stress cardiomyopathy	32.65	26.87	12	2122	11154	79731100
Congestive cardiomyopathy	32.02	26.87	12	2122	11768	79730486
Adenocarcinoma metastatic	29.44	26.87	5	2129	186	79742068
Cardiac failure	27.87	26.87	27	2107	154815	79587439

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	L01XX35	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS OTHER ANTINEOPLASTIC AGENTS Other antineoplastic agents
CHEBI has role	CHEBI:48675	antifibrinolytic agent
CHEBI has role	CHEBI:50427	platelet aggregation inhibitors
CHEBI has role	CHEBI:35554	cardiovascular agent
CHEBI has role	CHEBI:50249	anticoagulants
FDA EPC	N0000175638	Platelet-reducing Agent
FDA MoA	N0000175086	Phosphodiesterase 3 Inhibitors
FDA PE	N0000175972	Decreased Platelet Production
MeSH PA	D002317	Cardiovascular Agents
MeSH PA	D005343	Fibrinolytic Agents

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Drug Use | Suggest Off label Use Form| |View source of the data|

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Disease	Relation	SNOMED_ID	DOID
Essential thrombocythemia	indication	109994006	DOID:2224
Thrombocytosis in Myeloproliferative Disease	indication
High output heart failure	contraindication	10091002
Heart disease	contraindication	56265001	DOID:114
Hepatic failure	contraindication	59927004
Interstitial pneumonia	contraindication	64667001
Blood coagulation disorder	contraindication	64779008	DOID:1247
Kidney disease	contraindication	90708001	DOID:557
Interstitial lung disease	contraindication	233703007	DOID:3082
Disease of liver	contraindication	235856003	DOID:409

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🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	10.12	acidic
pKa2	3.82	Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
cGMP-inhibited 3',5'-cyclic phosphodiesterase A	Enzyme	Q14432	PDE3A_HUMAN	INHIBITOR	IC50	7.27		IUPHAR	CHEMBL
cGMP-dependent 3',5'-cyclic phosphodiesterase	Enzyme	O00408	PDE2A_HUMAN		IC50	4.47		CHEMBL

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External reference:

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ID	Source
006435	NDDF
006436	NDDF
108976008	SNOMEDCT_US
108977004	SNOMEDCT_US
135409400	PUBCHEM_CID
236612	RXNORM
372561005	SNOMEDCT_US
4021052	VANDF
4024077	VUID
4024077	VANDF

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Anagrelide Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0172-5240	CAPSULE	1 mg	ORAL	ANDA	26 sections
Anagrelide Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0172-5241	CAPSULE	0.50 mg	ORAL	ANDA	26 sections

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