Deslorelin is a synthetic peptide analogue of GnRH (gonadotropin-releasing hormone), a naturally occurring hormone that plays a key role in the regulation of reproductive functions. Deslorelin is specifically designed to have a longer duration of action in research compared to natural GnRH.
Deslorelin, a synthetic counterpart to gonadotropin-releasing hormone (GnRH), surpasses the natural hormone in potency and resistance to proteolysis. It binds to the anterior pituitary cell GnRH receptor with great affinity, just like GnRH does, and functions as an agonist there. It causes the anterior pituitary to secrete more LH and FSH when exposed acutely, but chronic, continuous exposure causes the pituitary gonadotropes to become desensitized, which potentially inhibits secretion. Similar to other GnRH agonists, it may find therapeutic use in the management of malignant neoplasms, endometriosis, uterine leiomyoma (fibroid tumors), and assisted reproductive procedures. Nowadays, it’s mostly utilized in veterinary medicine to promote ovulation in cows and mares. [R]
How Does Deslorelin Work?
Deslorelin has the potential to act on the pituitary gland to initially stimulate the release of two key reproductive hormones – follicle-stimulating hormone (FSH) and luteinizing hormone (LH). This surge of FSH and LH induces ovulation, follicular maturation, and sex hormone production in female and male dogs/cats. However, when given, in research, continuously at sustained doses over time, Deslorelin subsequently suppresses the reproductive system. Prolonged signaling causes downregulation of GnRH receptors in the pituitary, making gonadotroph cells less responsive to GnRH stimuli. This reduction in pituitary sensitivity inhibits further release of FSH and LH. Through this dual pattern of first activating and then desensitizing the pituitary-gonadal axis, sustained Deslorelin research treatment reversibly switches off reproductive function. Suppressed circulation of downstream sex hormones mediates both the potential contraceptive and therapeutic effects.
As a GnRH agonist, Deslorelin’s mechanism relies on transient stimulation followed by sustained reversible suppression of the hypothalamic-pituitary-gonadal hormonal cascade via modulation of pituitary GnRH receptor signaling. [R]
Deslorelin Potential Applications
Below are other research-based additional benefits Deslorelin brings:
Deslorelin and Potential Prostate Cancer Therapy
According to a study, Deslorelin conjugated with other chemotherapy compounds docetaxel, potentially enhanced the potency and efficacy of docetaxel against prostate cancer cells significantly. Results of the laboratory studies showed the deslorelin-docetaxel conjugate drug was over 15 times more potent than docetaxel alone at inhibiting prostate cancer cell proliferation. Additionally, linkage to deslorelin increased cancer cell death by 5-fold compared to treatment with docetaxel alone.[R]
In prostate tumor animal models, the deslorelin modification drastically improved the antitumor efficacy of docetaxel treatment. Tumor growth inhibition was amplified over 5.5 times. The greatly amplified overall antitumor activities suggest the deslorelin-docetaxel conjugate holds promise as a novel therapeutic strategy for prostate cancer. The targeted and enhanced effects demonstrate key health benefits of Deslorelin and justify further research on optimal utilization in cancer therapies. [R]
Deslorelin and Uterine Fibroids Research
In a clinical study, Deslorelin was evaluated for a period of six to twelve months in conjunction with add-back low-dose estrogen therapy to reduce the size and symptoms of uterine fibroids (UF), a non-cancerous tumor that grows in and around the womb (uterus). Deslorelin dramatically reduced pelvic pain in 82% of test subjects as compared to a placebo, and in 76% of test subjects, it reduced bleeding scores by more than 75%. When using Deslorelin, uterine volume decreased by 21% on average but increased when taking a placebo. In summary, Deslorelin combined with estrogen add-back therapy significantly reduced the size of the fibroid and significantly relieved symptoms like discomfort and heavy bleeding. The add-back stopped bone loss brought on by therapy.[R]
Deslorelin and Premature Puberty Research
Studies showed that Deslorelin can be a potential treatment for central precocious puberty. Precocious puberty often leads to short adult height if left untreated. Deslorelin works by potentially suppressing puberty, thereby slowing bone maturation, and allowing more time for growth. A long-term pilot study on 161 juvenile test subjects with precocious puberty found that treatment with Deslorelin for an average of 4 years improved final adult height compared to pretreatment predicted height. However, the final height did not reach the genetic height potential while still on treatment. These results indicate deslorelin has the potential to partially restore height loss from precocious puberty. [R]
Deslorelin and Prostatic Hyperplasia
In animal studies, Deslorelin acetate was shown to have the potential to reduce symptoms associated with benign prostatic hyperplasia (BPH). While clinical improvement occurred faster with the comparator drugs, the effects of Deslorelin were more prolonged. BPH symptoms remained controlled with deslorelin through the entire 36-week study duration with no relapses detected. In addition to efficacy, both deslorelin and other drugs demonstrated safety with only mild side effects observed. Overall health status was not negatively impacted. In summary, Deslorelin provides substantial health benefits for managing BPH. The induction of lasting clinical remission and lack of significant safety risks make it a potential therapeutic option for the control of BPH and relief of associated obstructive symptoms. The long-term effectiveness of Deslorelin highlights a key advantage over other medical alternatives for this condition. [R]
Deslorelin and Endometriosis Research
A clinical trial showed that Deslorelin was used as a potential medication in conjunction with low-dose estrogen to alleviate pelvic pain related to endometriosis. During six months of treatment, Deslorelin was found to dramatically lower scores for important endometriosis symptoms such as dyspareunia, dysmenorrhea, pelvic pain, tenderness, and induration. Deslorelin therapy significantly improved patient-reported outcomes in several quality-of-life dimensions. [R]
Significantly, Deslorelin alone did not produce any hypoestrogenic symptoms or limited safety indications. There were negligible changes in hot flashes and bone mineral density, and no endometrial hyperplasia was seen.
Combined with hormone add-back therapy, Deslorelin showed significant symptom relief for endometriosis while preserving a good safety record. More investigation and clinical development are necessary for this innovative therapeutic strategy to manage endometriosis. [R]
Deslorelin and Ovulation Research
Deslorelin is a synthetic hormone used in veterinary medicine to induce ovulation. It stimulates the pituitary gland to release luteinizing hormone (LH) and follicle-stimulating hormone (FSH), which are crucial for the reproductive cycle when administered as a single dose injection in research contexts. Deslorelin is hence potentially helpful for breeding management. While research on the pharmacological effects of Deslorelin has been limited, its mechanisms of action suggest it likely has similar benefits via hormonal regulation in different species. However, more studies are needed, and use requires veterinary supervision to ensure appropriate dosing. [R]
Deslorelin has been studied in female Tammar wallabies to be an effective and reversible form of contraception. The duration of the reproductive inhibition caused by a 5 mg Deslorelin implant varied, averaging 515 ± 87 days. The treatment works by reducing luteinizing hormone levels and stopping the wallabies from going through their usual reproductive cycles. The study showed that, although the treatment prevented pregnancies, it didn’t have any bad effects, and the effects were completely reversible. [R]
Deslorelin has the potential to offer safe, efficient, and reversible contraception in male and female domestic cats when administered for long-term fertility suppression. Research shows that a 4.7 mg, Deslorelin implant can suppress sex hormones for about 24 months in females and 20 months in males. This reversibility is shown by the fact that viable matings can occur about two years after treatment. Challenges include variability in the duration of suppression, the need for optimal reimplantation timing, and managing a temporary fertile phase. While additional controlled studies are warranted to address these challenges and assess the impact of repeated treatments on prepubertal cats, the ease of use and favorable characteristics of Deslorelin implants support their potential for effective and reversible control of feline reproduction. [R]
Deslorelin and Adrenocortical Disease (Acd)
Adrenocortical disease causes alopecia, swollen vulva in females, muscle atrophy, hind limb weakness, and sexual activity or aggression. Males can develop prostatic cysts, prostatitis, and urethral obstruction. As the disease progresses, there is often a decrease in the apparent quality of life.
In a study, Deslorelin implants significantly improved clinical signs of ACD in animal test subjects, including eliminating vulvar swelling, pruritus, sexual behaviors, and aggression within 14 days. Hair regrowth occurred after 4-6 weeks. Plasma steroid hormone levels also rapidly decreased within 1 month and remained lowered until relapse. These results demonstrate Deslorelin can potentially control symptoms and hormonal excess in ACD long-term. This makes it a potential treatment option for managing sequelae of the disease without the need for surgery/anesthesia. In summary, Deslorelin implants offer a potential option for controlling clinical and hormonal manifestations of ACD, providing prolonged benefits. However effects on tumor growth require further study, and clinical monitoring for relapse remains important.[R]
Deslorelin shows potential therapeutic promise for a range of illnesses. Deslorelin conjugated with other therapeutic drugs considerably increases potency and efficacy against prostate cancer cells in prostate cancer therapy, suggesting potential as a novel therapeutic approach. When studied in conjunction with estrogen add-back therapy, deslorelin reduces the size of uterine fibroids and greatly reduces associated symptoms, making it a useful potential future treatment choice. Deslorelin shows potential in slowing bone maturation and partially recovering height loss in cases with central precocious puberty. Deslorelin is superior to other options in treating benign prostatic hyperplasia because it offers long-lasting clinical remission and extended symptom alleviation. Deslorelin successfully lowers symptoms and enhances outcomes in endometriosis while retaining an excellent safety profile when coupled with low-dose estrogen. Deslorelin also shows promise in the management of Adrenocortical Disease by regulating clinical manifestations and hormonal excess. Overall, these findings emphasize the multifaceted potential health benefits of Deslorelin across diverse medical applications, warranting further research and clinical development.
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