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Ormeloxifene API Manufacturers & Suppliers

General Description:

Ormeloxifene, identified by CAS number 31477-60-8, is a notable compound with significant therapeutic applications. Ormeloxifene is a third-generation selective estrogen receptor (ER) modulator. In India, ormeloxifene has been marketed since the 1990s as a non-hormonal, non-steroidal oral contraceptive taken once a week, and it was later introduced for the treatment of dysfunctional uterine bleeding. Similar to other selective estrogen receptor modulators (SERMs), ormeloxifene has estrogenic activity in the vagina, bone, cardiovascular, and central nervous system tissues, and anti-estrogenic activity in the uterus and breast. The use of ormeloxifene for the treatment of perimenopausal bleeding and the management of menorrhagia has also been investigated. Ormeloxifene is marketed in India as a racemic mixture of the l- (levormeloxifene) and d-isomers (d-ormeloxifene) of _trans_-ormeloxifene. The use of levormeloxifene for the treatment of reduced bone turnover and the prevention of atherosclerosis has been evaluated; however, drug development was discontinued due to adverse events.

Metabolism:

Ormeloxifene undergoes metabolic processing primarily in: _In vivo_ studies suggest that ormeloxifene is quickly metabolized by the liver. In rats, the active metabolite of this drug is 7-desmethylated ormeloxifene. This metabolic pathway ensures efficient processing of the drug, helping to minimize potential toxicity and side effects.

Absorption:

The absorption characteristics of Ormeloxifene are crucial for its therapeutic efficacy: In healthy, non-lactating volunteers given 30 mg of ormeloxifene (n=11), the C_max, t_max and AUC_0-∞ were 55.5 ng/mL, 5.2 h, and 5199 ng⋅h/mL, respectively. The drug's ability to rapidly penetrate into cells ensures quick onset of action.

Half-life:

The half-life of Ormeloxifene is an important consideration for its dosing schedule: In healthy, non-lactating volunteers given 30 mg of ormeloxifene (n=11), the half-life is 165 h. This determines the duration of action and helps in formulating effective dosing regimens.

Protein Binding:

Ormeloxifene exhibits a strong affinity for binding with plasma proteins: Approximately 90% of ormeloxifene is bound to albumin. This property plays a key role in the drug's pharmacokinetics and distribution within the body.

Route of Elimination:

The elimination of Ormeloxifene from the body primarily occurs through: _In vivo_ studies suggest that ormeloxifene is excreted from the body primarily via feces. Understanding this pathway is essential for assessing potential drug accumulation and toxicity risks.

Volume of Distribution:

Ormeloxifene is distributed throughout the body with a volume of distribution of: In healthy women, the apparent volume of distribution (Vd/F) was higher than the total body fluid, and the nursing state does not have an effect on this parameter. This metric indicates how extensively the drug permeates into body tissues.

Clearance:

The clearance rate of Ormeloxifene is a critical factor in determining its safe and effective dosage: In healthy, non-lactating volunteers given 30 mg of ormeloxifene (n=11), the clearance is 0.14 L/h. It reflects the efficiency with which the drug is removed from the systemic circulation.

Pharmacodynamics:

Ormeloxifene exerts its therapeutic effects through: Ormeloxifene is a selective estrogen receptor modulator (SERMs) with contraceptive activity. Also, it has been suggested that it may be beneficial in the treatment of breast cancer, osteoporosis, dermatitis, restenosis, endometriosis and uterine fibroids. The drug's ability to modulate various physiological processes underscores its efficacy in treating specific conditions.

Mechanism of Action:

Ormeloxifene functions by: Ormeloxifene has both estrogenic and anti-estrogenic activity. As a contraceptive, ormeloxifene inhibits endometrial receptivity to blastocyst signals. This mechanism inhibits implantation without affecting nidatory estrogen and progesterone, the hypothalamo-pituitary-ovarian axis, follicle maturation, ovulation, mating behavior, gamete transport or fertilization, and the preimplantation development of embryos. This mechanism highlights the drug's role in inhibiting or promoting specific biological pathways, contributing to its therapeutic effects.

Toxicity:

Classification:

Ormeloxifene belongs to the class of organic compounds known as 7-o-methylated isoflavonoids. These are isoflavonoids with methoxy groups attached to the C7 atom of the isoflavonoid backbone. Isoflavonoids are natural products derived from 3-phenylchromen-4-one, classified under the direct parent group 7-O-methylated isoflavonoids. This compound is a part of the Organic compounds, falling under the Phenylpropanoids and polyketides superclass, and categorized within the Isoflavonoids class, specifically within the O-methylated isoflavonoids subclass.

Categories:

Ormeloxifene is categorized under the following therapeutic classes: Adrenal Cortex Hormones, Benzopyrans, Chromans, Contraceptive Agents, Female, Contraceptives, Oral, Contraceptives, Postcoital, Estrogen Antagonists, Genito Urinary System and Sex Hormones, Heterocyclic Compounds, Fused-Ring, Hormonal Contraceptives for Systemic Use, Hormone Antagonists, Hormones, Hormone Substitutes, and Hormone Antagonists, Pyrans, Reproductive Control Agents, Selective Estrogen Receptor Modulators, Sex Hormones and Modulators of the Genital System. These classifications highlight the drug's diverse therapeutic applications and its importance in treating various conditions.