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- Ormeloxifene
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Ormeloxifene | CAS No: 31477-60-8 | GMP-certified suppliers
A medication that provides non-steroidal oral contraception and treatment for dysfunctional uterine bleeding with selective estrogen receptor modulation benefits.
Therapeutic categories
Product Snapshot
- Ormeloxifene is an oral non-steroidal selective estrogen receptor modulator (SERM)
- Its primary therapeutic application is in contraception and as a treatment for certain gynecological conditions
- The compound currently holds an experimental status with no approved regulatory market authorizations
Clinical Overview
Clinically, ormeloxifene is primarily used in India as a non-hormonal, non-steroidal oral contraceptive administered once weekly. It has also been introduced for the treatment of dysfunctional uterine bleeding and has been investigated for indications such as perimenopausal bleeding and menorrhagia. Additional potential therapeutic areas under study include breast cancer, osteoporosis, dermatitis, restenosis, endometriosis, and uterine fibroids, although these uses remain experimental.
Pharmacodynamically, ormeloxifene exhibits tissue-selective estrogenic and anti-estrogenic effects. It acts as an estrogen receptor modulator, demonstrating estrogenic activity in vaginal, bone, cardiovascular, and central nervous system tissues, while exerting anti-estrogenic effects in the uterus and breast. Its contraceptive mechanism is attributed to the inhibition of endometrial receptivity to blastocyst implantation signals without disrupting ovulation, follicular development, gamete transport, or embryo preimplantation development. This action differentiates it from steroidal contraceptives that alter systemic hormone levels or ovulatory cycles.
Key pharmacokinetic attributes including absorption, distribution, metabolism, and excretion (ADME) parameters have not been comprehensively documented in publicly available sources. However, clinical use as a weekly oral agent suggests a suitable pharmacokinetic profile supporting sustained efficacy.
Safety considerations include known adverse events associated with the levormeloxifene isomer, which led to discontinuation of its development in indications such as bone turnover and atherosclerosis prevention. Comprehensive safety evaluation remains essential given ormeloxifene’s estrogen receptor modulation and its potential impacts on reproductive and other estrogen-sensitive tissues.
Notable usage contexts are primarily restricted to the Indian pharmaceutical market, where ormeloxifene is registered and marketed under various brand names for contraception and uterine bleeding disorders.
From an API sourcing perspective, quality assurance must ensure isomeric purity consistent with the racemic mixture and compliance with international pharmacopoeial standards. Reliable characterization of the 7-O-methylated isoflavonoid structure and impurity profiling are critical to maintain batch-to-batch consistency and regulatory compliance in global supply chains.
Identification & chemistry
| Generic name | Ormeloxifene |
|---|---|
| Molecule type | Small molecule |
| CAS | 31477-60-8 |
| UNII | 44AXY5VE90 |
| DrugBank ID | DB13310 |
Pharmacology
| Summary | Ormeloxifene is a selective estrogen receptor modulator (SERM) targeting estrogen receptor alpha and beta, exhibiting tissue-specific estrogenic and anti-estrogenic effects. Its contraceptive action is primarily mediated by inhibiting endometrial receptivity to blastocyst implantation without disrupting the hypothalamo-pituitary-ovarian axis or ovulation. Additionally, ormeloxifene demonstrates potential therapeutic effects across various estrogen-related conditions. |
|---|---|
| Mechanism of action | 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. |
| Pharmacodynamics | 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. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Estrogen receptor alpha | Humans | modulator |
| Estrogen receptor beta | Humans | modulator |
ADME / PK
| Absorption | In healthy, non-lactating volunteers given 30 mg of ormeloxifene (n=11), the C<sub>max</sub>, t<sub>max</sub> and AUC<sub>0-∞</sub> were 55.5 ng/mL, 5.2 h, and 5199 ng⋅h/mL, respectively. |
|---|---|
| Half-life | In healthy, non-lactating volunteers given 30 mg of ormeloxifene (n=11), the half-life is 165 h. |
| Protein binding | Approximately 90% of ormeloxifene is bound to albumin. |
| Metabolism | _In vivo_ studies suggest that ormeloxifene is quickly metabolized by the liver. In rats, the active metabolite of this drug is 7-desmethylated ormeloxifene. |
| Route of elimination | _In vivo_ studies suggest that ormeloxifene is excreted from the body primarily via feces. |
| Volume of distribution | 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. |
| Clearance | In healthy, non-lactating volunteers given 30 mg of ormeloxifene (n=11), the clearance is 0.14 L/h. |
Formulation & handling
- Ormeloxifene is a small molecule primarily intended for oral administration due to its physicochemical properties.
- High lipophilicity (LogP 6.03) and low water solubility indicate challenges in aqueous formulation and potential need for solubilization strategies.
- Stability considerations include protection from moisture and light due to its experimental status and low aqueous solubility.
Regulatory status
Safety
| Toxicity | Toxicity information regarding ormeloxifene is not readily available. Patients experiencing an overdose are at an increased risk of severe cardiovascular adverse effects. Symptomatic and supportive measures are recommended. |
|---|
- Ormeloxifene has limited publicly available toxicity data
- Handle with standard precautions to minimize exposure
- In cases of overdose, severe cardiovascular effects may occur
Ormeloxifene is a type of Genitourinary Agents
Genitourinary agents are a category of pharmaceutical active ingredients (APIs) that are specifically designed to target and treat disorders related to the genitourinary system. The genitourinary system encompasses the organs and structures involved in the production, storage, and elimination of urine, as well as the reproductive organs.
These APIs play a crucial role in the treatment of various genitourinary conditions, including urinary tract infections (UTIs), erectile dysfunction, urinary incontinence, benign prostatic hyperplasia (BPH), and other related disorders. They exert their therapeutic effects by interacting with specific receptors or enzymes in the genitourinary system, regulating physiological processes, and restoring normal function.
Some commonly used genitourinary agents include alpha-blockers, which relax the smooth muscles in the prostate and bladder neck, improving urine flow in patients with BPH. Additionally, phosphodiesterase type 5 inhibitors (PDE5 inhibitors) are widely prescribed for erectile dysfunction, as they enhance blood flow to the penile tissues, facilitating erection.
These APIs are typically formulated into various dosage forms, such as tablets, capsules, creams, gels, or injections, allowing for convenient administration to patients. The development and production of genitourinary agents involve stringent quality control measures and compliance with regulatory guidelines to ensure safety, efficacy, and consistent product performance.
In summary, genitourinary agents form a crucial category of pharmaceutical APIs used to treat a range of disorders affecting the genitourinary system. Their targeted mechanisms of action and diverse dosage forms make them valuable tools in improving genitourinary health and enhancing patients' quality of life.
