- Molecular NameNafarelin
- SynonymNafarelin acetate
- Weight1322.5
- Drugbank_IDDB00666
- ACS_NO76932-56-4
- Show 3D model
- LogP (experiment)N/A
- LogP (predicted, AB/LogP v2.0)N/A
- pkaN/A
- LogD (pH=7, predicted)N/A
- Solubility (experiment)N/A
- LogS (predicted, ACD/Labs)(ph=7)N/A
- LogSw (predicted, AB/LogsW2.0)N/A
- Sw (mg/ml) (predicted, ACD/Labs)N/A
- No.of HBond DonorsN/A
- No.of HBond AcceptorsN/A
- No.of Rotatable BondsN/A
- TPSAN/A
- StatusFDA approved
- AdministrationNasal spray
- PharmacologyA gonadotropin-releasing hormone agonist (GnRH agonist) which acts as an analog of GnRH. Nafarelin increases the release of FSH and LH by the anterior pituitary, which in turn leads to an increase of estrogen/progesterone. When administered, Nafarelin has the purpose of causing increase estrogen that will negatively feed back upon hypothalamus to decrease GnRH ( negative feedback loop ) Through negative feedback, Nafarelin causes a decrease in pituitary secretion of gonadotropins luteinizing hormone (LH) and follicle stimulating hormone (FSH). Nafarelin may be used in the treatment of estrogen-dependent conditions (such as endometriosis or uterine fibroids), to treat central precocious puberty, and to control ovarian stimulation in IVF.
- Absorption_value0.0
- Absorption (description)N/A
- Caco_2N/A
- BioavailabilityN/A
- Protein binding81.0
- Volume of distribution (VD)N/A
- Blood/Plasma Partitioning ratio (D_blood)N/A
- MetabollsmEnzymatic hydrolysis.
- Half life3~4 h (intranasal administration). Also reported as 2.0 to 2.7 h after subcutaneous and intranasal administration.
- Excretionrenal
- Urinary ExcretionN/A
- CleranceN/A
- ToxicityN/A
- LD50 (rat)N/A
- LD50 (mouse)N/A