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

Stem definition	Drug id	CAS RN
	1399	127-07-1

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: xromi siklos hydroxyurea biosupressin carbamohydroxamic acid carbamohydroximic acid carbamoyl oxime oxyrea oxyurea hydroxycarbamide	An antineoplastic agent that inhibits DNA synthesis through the inhibition of ribonucleoside diphosphate reductase. Molecular weight: 76.06 Formula: CH4N2O2 CLOGP: -1.80 LIPINSKI: 0 HAC: 4 HDO: 3 TPSA: 75.35 ALOGS: 0.55 ROTB: 0

Molecule

Description

Molfile Inchi Smiles

Synonyms:

xromi
siklos
hydroxyurea
biosupressin
carbamohydroxamic acid
carbamohydroximic acid
carbamoyl oxime
oxyrea
oxyurea
hydroxycarbamide

An antineoplastic agent that inhibits DNA synthesis through the inhibition of ribonucleoside diphosphate reductase.

Molecular weight: 76.06
Formula: CH4N2O2
CLOGP: -1.80
LIPINSKI: 0
HAC: 4
HDO: 3
TPSA: 75.35
ALOGS: 0.55
ROTB: 0

Drug dosage:

None

ADMET properties:

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Property	Value	Reference
EoM (Fraction excreted unchanged in urine)	80 %	Benet LZ, Broccatelli F, Oprea TI
BA (Bioavailability)	79 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
S (Water solubility)	50 mg/mL	Benet LZ, Broccatelli F, Oprea TI
t_half (Half-life)	3.40 hours	Lombardo F, Berellini G, Obach RS
BDDCS (Biopharmaceutical Drug Disposition Classification System)	3	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	1502.57 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
CL (Clearance)	1.50 mL/min/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	1 %	Lombardo F, Berellini G, Obach RS
Vd (Volume of distribution)	0.52 L/kg	Lombardo F, Berellini G, Obach RS

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Approvals:

Date	Agency	Company	Orphan
Dec. 7, 1967	FDA	BRISTOL MYERS SQUIBB
July 1, 2019	EMA	NOVA LABORATORIES 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
Sickle cell anaemia with crisis	710.26	14.09	187	16348	5816	63466671
Platelet count increased	276.06	14.09	120	16415	17591	63454896
Acute myeloid leukaemia	176.02	14.09	87	16448	17060	63455427
Acute chest syndrome	164.30	14.09	39	16496	782	63471705
Splenomegaly	155.77	14.09	70	16465	11087	63461400
Myelofibrosis	125.72	14.09	35	16500	1342	63471145
White blood cell count increased	117.58	14.09	99	16436	48462	63424025
Thrombocytopenia	105.58	14.09	161	16374	150996	63321491
Haemoglobin decreased	104.51	14.09	157	16378	145328	63327159
Blast crisis in myelogenous leukaemia	98.77	14.09	24	16511	533	63471954

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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
Sickle cell anaemia with crisis	635.07	14.25	178	16015	3875	34936863
Acute myeloid leukaemia	158.15	14.25	101	16092	18169	34922569
Myelofibrosis	148.53	14.25	47	16146	1564	34939174
Differentiation syndrome	145.31	14.25	45	16148	1393	34939345
Acute chest syndrome	137.12	14.25	38	16155	789	34939949
Splenomegaly	126.93	14.25	82	16111	15035	34925703
Blast crisis in myelogenous leukaemia	124.73	14.25	33	16160	571	34940167
Chronic myeloid leukaemia	114.81	14.25	42	16151	2182	34938556
White blood cell count increased	112.84	14.25	116	16077	41035	34899703
Tumour lysis syndrome	104.08	14.25	76	16117	16983	34923755

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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
Sickle cell anaemia with crisis	1051.58	13.18	286	26907	7636	79709559
Acute myeloid leukaemia	280.83	13.18	158	27035	30727	79686468
Acute chest syndrome	272.15	13.18	70	27123	1491	79715704
Platelet count increased	223.89	13.18	122	27071	22284	79694911
Differentiation syndrome	217.02	13.18	65	27128	2459	79714736
Splenomegaly	207.35	13.18	113	27080	20641	79696554
Myelofibrosis	204.70	13.18	62	27131	2438	79714757
Blast crisis in myelogenous leukaemia	176.15	13.18	44	27149	829	79716366
Thrombocytopenia	155.80	13.18	304	26889	264955	79452240
White blood cell count increased	148.99	13.18	154	27039	74479	79642716

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	L01XX05	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS OTHER ANTINEOPLASTIC AGENTS Other antineoplastic agents
CHEBI has role	CHEBI:35221	antimetabolite
CHEBI has role	CHEBI:35610	antineoplastic agents
CHEBI has role	CHEBI:48578	free radical scavengers
CHEBI has role	CHEBI:50846	Immunologic factor
CHEBI has role	CHEBI:50902	genotoxic agent
CHEBI has role	CHEBI:50905	teratogeno
CHEBI has role	CHEBI:59517	DNA synthesis inhibitors
CHEBI has role	CHEBI:64911	mitotic inhibitor
CHEBI has role	CHEBI:74213	EC 1.17.4.1 inhibitor

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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
Chronic myeloid leukemia	indication	92818009	DOID:8552
Hb SS disease	indication	127040003	DOID:10923
Malignant tumor of head and/or neck	indication	255056009
Malignant tumor of ovary	indication	363443007	DOID:2394
Malignant melanoma	indication	372244006
Sickling disorder due to hemoglobin S	indication	417357006
Hemoglobin SS disease with crisis	indication	417425009
Polycythemia vera	off-label use	109992005
Essential thrombocythemia	off-label use	109994006	DOID:2224
Vasculitis of the skin	contraindication	53312001

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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	10.38	acidic
pKa2	12.5	acidic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
100MG	SIKLOS	ADDMEDICA SAS	N208843	Dec. 21, 2017	RX	TABLET	ORAL	Dec. 21, 2024	TO REDUCE THE FREQUENCY OF PAINFUL CRISES AND TO REDUCE THE NEED FOR BLOOD TRANSFUSIONS IN PEDIATRIC PATIENTS, 2 YEARS OF AGE AND OLDER, WITH SICKLE CELL ANEMIA WITH RECURRENT MODERATE TO SEVERE PAINFUL CRISIS
1GM	SIKLOS	ADDMEDICA SAS	N208843	Dec. 21, 2017	RX	TABLET	ORAL	Dec. 21, 2024	TO REDUCE THE FREQUENCY OF PAINFUL CRISES AND TO REDUCE THE NEED FOR BLOOD TRANSFUSIONS IN PEDIATRIC PATIENTS, 2 YEARS OF AGE AND OLDER, WITH SICKLE CELL ANEMIA WITH RECURRENT MODERATE TO SEVERE PAINFUL CRISIS

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Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Ribonucleoside-diphosphate reductase large subunit	Enzyme	P23921	RIR1_HUMAN	INHIBITOR			WOMBAT-PK	CHEMBL
Ribonucleoside-diphosphate reductase subunit M2	Enzyme	P31350	RIR2_HUMAN	INHIBITOR			WOMBAT-PK	CHEMBL
Carbonic anhydrase 2	Enzyme	P00918	CAH2_HUMAN		Ki	4.55	CHEMBL
Carbonic anhydrase 9	Enzyme	Q16790	CAH9_HUMAN		Ki	4.64	CHEMBL
Carbonic anhydrase 5A, mitochondrial	Enzyme	P35218	CAH5A_HUMAN		Ki	4.51	CHEMBL

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External reference:

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ID	Source
002635	NDDF
148307	MMSL
1763	MMSL
1991	INN_ID
1999309	RXNORM
3657	PUBCHEM_CID
387314007	SNOMEDCT_US
4017733	VUID
4017733	VANDF
4856	MMSL

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
DROXIA	HUMAN PRESCRIPTION DRUG LABEL	1	0003-6335	CAPSULE	200 mg	ORAL	NDA	29 sections
DROXIA	HUMAN PRESCRIPTION DRUG LABEL	1	0003-6335	CAPSULE	200 mg	ORAL	NDA	29 sections
DROXIA	HUMAN PRESCRIPTION DRUG LABEL	1	0003-6336	CAPSULE	300 mg	ORAL	NDA	29 sections
DROXIA	HUMAN PRESCRIPTION DRUG LABEL	1	0003-6336	CAPSULE	300 mg	ORAL	NDA	29 sections
DROXIA	HUMAN PRESCRIPTION DRUG LABEL	1	0003-6337	CAPSULE	400 mg	ORAL	NDA	29 sections
DROXIA	HUMAN PRESCRIPTION DRUG LABEL	1	0003-6337	CAPSULE	400 mg	ORAL	NDA	29 sections
DROXIA	HUMAN PRESCRIPTION DRUG LABEL	1	61269-402	CAPSULE	200 mg	ORAL	NDA	29 sections
DROXIA	HUMAN PRESCRIPTION DRUG LABEL	1	61269-402	CAPSULE	200 mg	ORAL	NDA	29 sections
DROXIA	HUMAN PRESCRIPTION DRUG LABEL	1	61269-403	CAPSULE	300 mg	ORAL	NDA	29 sections
DROXIA	HUMAN PRESCRIPTION DRUG LABEL	1	61269-403	CAPSULE	300 mg	ORAL	NDA	29 sections

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