Synonym |
(D-His2,D-Trp6)-LHRH |
Species |
Human |
Protein Accession |
P01148 |
Purity |
Greater than 95% |
Endotoxin Level |
Less than 1 EU/µg |
Biological Activity |
Not specified |
Expression System |
Chemical Synthesis |
Fusion Tag |
None |
Predicted Molecular Mass |
1182.4 Da |
Formulation |
Lyophilized from a 0.2 µm filtered solution in Acetonitrile and TFA |
Reconstitution |
Reconstitute in water to a concentration of 0.1-1.0 mg/ml. |
Storage & Stability |
Store lyophilized product at -20°C. Reconstituted product is stable for up to 1 week at 4°C and
for up to 3 months at -20°C. |
FAQ
What is (D-His2,D-Trp6)-LHRH and how does it work in the body?
(D-His2,D-Trp6)-LHRH is a synthetic
peptide that acts as an analog of the naturally occurring luteinizing hormone-releasing hormone (LHRH),
also known as gonadotropin-releasing hormone (GnRH). This analog is specially designed to interact with
the pituitary gland, which is responsible for regulating hormones related to reproductive processes. In
a typical physiological context, LHRH is released by the hypothalamus and travels to the pituitary
gland, where it stimulates the release of two primary gonadotropins: luteinizing hormone (LH) and
follicle-stimulating hormone (FSH). These hormones are crucial for reproductive functions in both males
and females. However, (D-His2,D-Trp6)-LHRH works in a unique manner. By acting as an agonist, it
over-stimulates the LHRH receptors in the pituitary gland, which initially causes an increase in LH and
FSH secretion. However, with continued stimulation, there is a paradoxical effect—a downregulation or
desensitization of the receptors occurs, leading to a decrease in the production and release of both LH
and FSH. This ultimately results in a reduction in the levels of sex hormones like testosterone in men
and estrogen in women. The compound's primary utility lies in its ability to effectively lower these
hormone levels, making it useful in clinical settings for conditions that are either exacerbated or
caused by high levels of sex hormones. Such conditions include hormone-sensitive cancers like prostate
cancer in men and breast cancer in women, as well as other hormone-related disorders.
What are
the primary applications of (D-His2,D-Trp6)-LHRH in medical treatment?
The primary applications of
(D-His2,D-Trp6)-LHRH are largely centered around its ability to manage hormone levels within the body,
which can be extremely beneficial for several clinical conditions. One of the most prominent uses of
this peptide analog is in the treatment and management of hormone-dependent cancers—most notably,
prostate cancer in men and breast cancer in women. In the case of prostate cancer, reducing testosterone
levels can help in suppressing tumor growth and slowing down the progression of the disease, as prostate
cancer cells typically rely on testosterone to grow and spread. For breast cancer, particularly in
postmenopausal women, similar principles apply with estrogen; by decreasing estrogen levels, it may be
possible to limit cancer progression and support other treatment modalities. Furthermore,
(D-His2,D-Trp6)-LHRH is sometimes used in the treatment of endometriosis, a painful condition where
tissue similar to the uterine lining grows outside the uterus, potentially benefiting from lowered
estrogen levels that reduce symptoms and lesion size. The compound is also applied in the context of in
vitro fertilization (IVF) and assisted reproductive technologies (ART), where it is used to carefully
control ovarian stimulation by initially suppressing the natural hormonal cycle, thus allowing for more
controlled stimulation and increased egg yield at a later stage. This capacity to manipulate
reproductive hormones is crucial for optimizing the timing and success rates of such procedures.
Additionally, (D-His2,D-Trp6)-LHRH might be used in certain cases of precocious puberty to delay the
onset of early puberty and give children more time for growth and development. The versatility and
effectiveness of (D-His2,D-Trp6)-LHRH in these varied applications underscore its valuable role in
modern medical treatment protocols.
Are there any known side effects or risks associated with
the use of (D-His2,D-Trp6)-LHRH?
Like any medical intervention, the use of (D-His2,D-Trp6)-LHRH does
come with the potential for side effects, which should be carefully weighed against its therapeutic
benefits. Initially, patients may experience what is known as a "flare effect." This is a transient
increase in sex hormones resulting from the initial overstimulation of the pituitary gland before
receptor downregulation occurs. For instance, in men undergoing treatment for prostate cancer, this can
lead to a temporary worsening of cancer symptoms, such as bone pain or urinary issues. To mitigate the
"flare effect," adjunct therapies, such as anti-androgens, may sometimes be employed. As the treatment
progresses and hormone levels begin to diminish, a range of symptoms related to hypoestrogenism in women
or low testosterone levels in men may emerge. In women, common side effects can include hot flashes,
night sweats, mood changes, vaginal dryness, and an increased risk of osteoporosis due to lowered
estrogen levels. Men, on the other hand, may experience symptoms such as reduced libido, erectile
dysfunction, fatigue, hot flashes, decrease in muscle mass, and potential risk of osteoporosis as a
result of decreased testosterone. Furthermore, long-term use of (D-His2,D-Trp6)-LHRH can have broader
implications on bone density and cardiovascular health due to the persistent lowering of sex hormones,
emphasizing the need for monitoring and potentially integrating supportive measures such as calcium and
vitamin D supplementation or addressing lifestyle factors that promote bone health. Patients with a
history of or at risk for cardiovascular disease should be monitored closely, as changes in hormone
levels can sometimes impact metabolic profiles and cardiovascular function. It's essential for patients
to maintain close communication with healthcare providers, allowing for symptom management and timely
adjustments to therapy to minimize side effects while optimizing therapeutic outcomes.
How does
(D-His2,D-Trp6)-LHRH compare to other hormone therapy treatments?
(D-His2,D-Trp6)-LHRH is part of a
broader class of treatments known as LHRH agonists, which are extensively used in hormone therapy
targeting various conditions reliant on the modulation of sex hormones. Comparatively, LHRH agonists
like (D-His2,D-Trp6)-LHRH offer distinct advantages and differences when considered alongside other
hormone therapy approaches, such as LHRH antagonists, anti-androgens, or aromatase inhibitors. Unlike
LHRH antagonists, which inhibit LHRH receptors more directly and rapidly reduce hormone levels, LHRH
agonists follow a two-phase hormone release—a temporary flare followed by suppression. This
characteristic requires additional management strategies to offset potential temporary exacerbations of
symptoms. Those opting for LHRH agonist treatments benefit from potentially favorable impacts on
hormone-sensitive tumors, though proper timing and adjunct therapies are crucial to minimizing adverse
effects. Anti-androgens, often used in conjunction with LHRH therapies to help manage prostate cancer,
particularly target androgen receptors at the tissue level, preventing testosterone from exerting its
effects. This mechanism complements the action of LHRH agonists, such as (D-His2,D-Trp6)-LHRH, by
providing a more comprehensive blockade of androgen activity when combined. In managing conditions like
breast cancer, aromatase inhibitors work prevalently by blocking the conversion of androgens into
estrogen in peripheral tissues, effectively reducing estrogen levels in postmenopausal women. However,
like (D-His2,D-Trp6)-LHRH, these can pose risks to bone health, necessitating vigilant monitoring and
prophylactic measures. Compared to surgical options like orchiectomy (removal of the testes) or
oophorectomy (removal of the ovaries), which irreversibly reduce hormone levels, (D-His2,D-Trp6)-LHRH
offers a reversible alternative, allowing for more flexibility in managing treatment duration and
intensity. Each of these therapies carries distinct benefit-risk profiles, justifying personalized
consideration to tailor treatment strategies based on individual patient health status, disease
progression, tolerability, and personal preferences. Collaboration between healthcare providers and
patients is pivotal in opting for an appropriate treatment path tailored to achieve the utmost efficacy
while mitigating potential side effects associated with hormone modulation.
Can
(D-His2,D-Trp6)-LHRH be used in fertility treatments, and if so, how does it contribute to success
rates?
Yes, (D-His2,D-Trp6)-LHRH has applications in fertility treatments, specifically in assisted
reproductive technologies like in vitro fertilization (IVF). In this context, it plays a crucial role in
controlling and optimizing the hormonal environment to increase the likelihood of successful conception.
One of the key challenges in fertility treatments is the ability to manage ovarian function and egg
maturation effectively. (D-His2,D-Trp6)-LHRH is employed before the planned stimulation phase to
suppress the natural luteinizing hormone (LH) surge. By doing so, it prevents premature ovulation,
allowing for greater control over the timing and quality of egg retrieval. The compound ensures that
multiple eggs can be harvested during a single cycle, enhancing the number of embryos available for
selection and thereby, improving the chances of implantation and successful pregnancy. Additionally, by
regulating the onset of ovulation, (D-His2,D-Trp6)-LHRH ensures that egg maturation is synchronized with
the fertility treatment timetable, which is crucial for adapting the cycle based on patient responses
and needs. By creating a more predictable and uniform response to ovarian stimulation, the reliability
and efficiency of fertility treatments are significantly improved. Moreover, (D-His2,D-Trp6)-LHRH
reduces the risk of ovarian hyperstimulation syndrome (OHSS) by allowing for a more controlled response
to stimulation, which is a common risk factor in fertility treatments due to excessive hormonal
stimulation. In this manner, the strategic use of (D-His2,D-Trp6)-LHRH can contribute to safer treatment
protocols, leading to a balance between higher efficacy and lower complication risks. It must be noted,
however, that the use of this compound in fertility treatments requires careful monitoring and
customization by healthcare providers to fit the unique hormonal profiles and reproductive needs of each
patient. Through a finely tuned balance of hormonal suppression and stimulation, (D-His2,D-Trp6)-LHRH
remains a pivotal component of personalized fertility treatment protocols, dedicated to increasing the
odds of success while prioritizing patient safety and comfort throughout the reproductive journey.