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Details

Stereochemistry ACHIRAL
Molecular Formula CH4N2O2
Molecular Weight 76.0547
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of Hydroxyurea

SMILES

NC(=O)NO

InChI

InChIKey=VSNHCAURESNICA-UHFFFAOYSA-N
InChI=1S/CH4N2O2/c2-1(4)3-5/h5H,(H3,2,3,4)

HIDE SMILES / InChI

Description

Hydroxyurea is an oral antimetabolite; inhibits ribonucleotide reductase and DNA synthesis. It is used for resistant chronic myeloid leukemia, locally advanced squamous cell carcinomas of the head and neck (excluding lip) in combination with concurrent chemoradiation, and to reduce the frequency of painful crises and the need for blood transfusions in patients with sickle cell anemia with recurrent moderate to severe painful crises. Hydroxyurea, a myelosuppressive agent, is the only effective drug proven to reduce the frequency of painful episodes. It raises the level of HbF and the haemoglobin level. It usually decreases the rate of painful episodes by 50%. It was first tested in sickle cell disease in 1984. It also decreases the rate of ACS episodes and blood transfusions by ~50 % in adults. It was developed as an anticancer drug and has been used to treat myeloproliferative syndromes-leukemia, melanoma, and ovarian cancer. It was approved for use by FDA in adults. Side effects includes neutropenia, bone marrow suppression, elevation of hepatic enzymes, anorexia, nausea, vomiting and infertility.

Approval Year

Targets

Primary TargetPharmacologyConditionPotency

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
DROXIA

Cmax

ValueDoseCo-administeredAnalytePopulation
793.75 μM
2000 mg single, oral
HYDROXYUREA plasma
Homo sapiens

AUC

ValueDoseCo-administeredAnalytePopulation
3934 μM × h
2000 mg single, oral
HYDROXYUREA plasma
Homo sapiens

T1/2

ValueDoseCo-administeredAnalytePopulation
3.32 h
2000 mg single, oral
HYDROXYUREA plasma
Homo sapiens

Doses

AEs

Drug as perpetrator​

Drug as victim

Tox targets

PubMed

Sample Use Guides

In Vivo Use Guide
Usual Adult Dose for Chronic Myelogenous Leukemia 15 mg/kg/day orally as a single dose Usual Adult Dose for Head and Neck Cancer 15 mg/kg/day orally as a single dose Usual Adult Dose for Sickle Cell Anemia 15 mg/kg orally once a day; increase 5 mg/kg/day every 12 weeks Maximum dose: 35 mg/kg/day Usual Pediatric Dose for Sickle Cell Anemia 2 years and older: 20 mg/kg orally once a day; increase 5 mg/kg/day every 8 weeks or if a painful crisis occurs; increase dosing only if blood counts are in the acceptable range; do not increase dosing if myelosuppression occurs; if blood counts are considered toxic, discontinue therapy until hematologic recovery Duration of therapy: Give until mild myelosuppression (absolute neutrophil count 2000/microliter to 4000/microliter) is achieved, up to 35 mg/kg/day Maximum dose: 35 mg/kg/day
Route of Administration: Oral