Synonym |
Trp6-LHRH |
Species |
Human |
Protein Accession |
P01148 |
Purity |
≥ 95% |
Endotoxin Level |
< 1.0 EU per μg |
Biological Activity |
Measured by its ability to inhibit secretion of FSH by rat pituitary cells. The ED50 for this
effect is typically 2-10 ng/mL. |
Expression System |
E. coli |
Fusion Tag |
None |
Predicted Molecular Mass |
Approximately 13928 Da |
Formulation |
Lyophilized from a 0.2 μm filtered solution of 20mM Acetic Acid, 250mM NaCl |
Reconstitution |
It is recommended to reconstitute the lyophilized Trp6-LHRH in sterile 18MΩ-cm H2O not less than
100 µg/ml, which can then be further diluted to other aqueous solutions. |
Storage & Stability |
Store at -20°C. Stable for 12 months from the date of receipt when stored at -20°C. |
FAQ
What is (Trp6)-LHRH and how does it work in the body?
(Trp6)-LHRH, also known as luteinizing
hormone-releasing hormone, is a synthetic analog of a naturally occurring hormone that plays a critical
role in the endocrine system. It functions as a regulatory hormone of the anterior pituitary gland and
is primarily involved in the control of reproductive hormone secretion. Naturally, LHRH prompts the
pituitary gland to release two other pivotal hormones: luteinizing hormone (LH) and follicle-stimulating
hormone (FSH). These hormones are crucial in regulating various reproductive processes, such as
ovulation in females and spermatogenesis in males. The synthetic form of LHRH, like (Trp6)-LHRH, is
engineered to have a more robust and sustained activity in the body compared to the natural hormone,
making it potentially more effective for specific medical applications.
Upon administration,
(Trp6)-LHRH binds to receptors located on the surface of the pituitary gland. The binding interaction
mimics the activity of natural LHRH. This binding stimulates the release of LH and FSH, key hormones
necessary for regulating the gonads—ovaries in females and testes in males. The increased levels of
these hormones can have a wide range of effects depending on the physiological context. In therapeutic
settings, (Trp6)-LHRH can be used to treat various reproductive health issues, including
hormone-sensitive cancers like prostate or breast cancer. In these cases, the administration of
(Trp6)-LHRH analogs can lead to a temporary surge in hormones, often followed by a down-regulation of
the LHRH receptors, ultimately leading to decreased levels of the sex hormones testosterone and
estrogen. This mechanism can help slow the progression of hormone-dependent tumors.
Moreover, the
structure of (Trp6)-LHRH has been modified to resist enzymatic degradation, thereby enhancing its
functional half-life in the bloodstream, allowing for more sustained therapeutic actions. This stability
ensures that the hormone remains active longer in the system and exhibits its desired effects over an
extended period. Understanding the mechanism of action of (Trp6)-LHRH provides insight into its
utilization in both clinical and research-based settings, highlighting its significance in advancing
treatments that rely on hormone regulation.
How is (Trp6)-LHRH used in clinical settings for
medical treatments?
In clinical settings, (Trp6)-LHRH is utilized primarily for its ability to
regulate reproductive hormones effectively. Its application spans several areas of medicine,
particularly in treating conditions related to hormone imbalances or hormone-sensitive disorders. One of
the most prominent uses of (Trp6)-LHRH analogs is in the treatment of prostate cancer. For advanced
prostate cancer, reducing the levels of testosterone is a primary goal, as this hormone can fuel the
growth of cancerous cells. (Trp6)-LHRH analogs are used to achieve chemical castration by initially
stimulating and then significantly suppressing testosterone production. This hormonal manipulation is
effective in slowing down or even stopping the progression of prostate cancer.
Another
significant application is in the treatment of breast cancer that is sensitive to hormonal regulation.
Estrogen can promote the growth of some breast cancer types, and reducing its levels in the body can be
an effective treatment strategy. By utilizing (Trp6)-LHRH analogs to downregulate the production of
hormones in the ovaries, clinicians can effectively reduce the amount of circulating estrogen, thereby
impacting cancer growth positively.
Beyond oncology, (Trp6)-LHRH is used in managing precocious
puberty, a condition where children experience early onset puberty. By administering (Trp6)-LHRH
analogs, healthcare providers can delay further development, allowing a child to grow at a more normal
developmental pace. The treatment involves suppressing the premature secretion of gonadotropins, which
are responsible for triggering puberty-related hormonal changes.
Additionally, (Trp6)-LHRH
analogs have applications in fertility treatments. By controlling hormone levels, physicians can create
an optimal environment for assisted reproductive technologies such as in vitro fertilization (IVF). In
this context, the analogs help synchronize the development of multiple follicles to increase the chances
of successful fertilization and pregnancy.
It is important to note that the use of (Trp6)-LHRH
should be carefully monitored by healthcare professionals. The dosing and administration are typically
tailored to the individual needs and medical history of the patient to ensure efficacy and reduce
potential side effects. Patients receiving this treatment are often monitored for hormone levels and
other parameters to gauge response and adjust therapy as needed.
What are the potential side
effects or adverse reactions when using (Trp6)-LHRH?
While (Trp6)-LHRH analogs are effective in
regulating hormone-related conditions, their use may come with certain side effects and adverse
reactions. These reactions are mainly due to the systemic changes in hormone levels that occur following
the administration of the analogs. One of the most common side effects is the initial surge in hormone
levels, which can lead to a temporary exacerbation of symptoms. This is often referred to as "flare,"
particularly in the context of prostate cancer treatment. During this period, patients may experience
worsening of symptoms like bone pain or urinary difficulties.
Additionally, the sustained
suppression of hormonal activity can lead to other significant physiological changes. For instance, in
both men and women, long-term use of (Trp6)-LHRH can result in symptoms associated with decreased sex
hormones such as hot flashes, decreased libido, fatigue, mood swings, and weight gain. In men, reduced
testosterone levels due to (Trp6)-LHRH treatment may lead to erectile dysfunction or loss of muscle
mass. In women, decreased estrogen levels may result in vaginal dryness, issues with vaginal health, and
an increased risk of osteoporosis.
The changes in bone density are particularly concerning since
prolonged suppression of sex hormones can weaken bones, making them more susceptible to fractures. As a
preventive measure, healthcare providers may recommend lifestyle changes, dietary adjustments, or
supplementation with calcium and vitamin D to mitigate these effects.
Furthermore, patients might
experience localized reactions at the injection site, such as pain, redness, or swelling. Systemically,
some might develop allergic reactions that can present as rash, itching, dizziness, or more severe cases
such as anaphylaxis, although these are rare. It's crucial for patients to inform their healthcare
provider if they experience any of these side effects so that appropriate measures can be taken, such as
dose adjustment or symptomatic treatment.
It's also important to understand that the propensity
for side effects varies among individuals. Factors such as the specific medical condition being treated,
the dosage of (Trp6)-LHRH, the duration of treatment, and the overall health status of the patient can
influence which side effects may occur and how severe they might be. Regular monitoring by healthcare
providers is essential in managing any side effects and ensuring the continued safety and efficacy of
the treatment. By keeping a close watch on their health and maintaining open communication with their
healthcare providers, patients can better navigate the potential challenges that come with (Trp6)-LHRH
therapy.
Can (Trp6)-LHRH help with any non-cancerous medical conditions?
Yes, (Trp6)-LHRH
can be utilized in the treatment of several non-cancerous medical conditions, particularly those related
to the reproductive system and hormone regulation. One of the notable non-cancerous conditions that
(Trp6)-LHRH is used to treat is precocious puberty. This condition involves the early onset of puberty
in children - before age 8 in girls and age 9 in boys. Administration of (Trp6)-LHRH analogs to children
with precocious puberty can help delay further sexual development until an appropriate age. The
mechanism involves suppressing the premature release of gonadotropins, effectively halting the premature
triggering of puberty-related hormonal changes. This delay allows affected children to achieve a more
normal growth and development trajectory, both physically and emotionally.
Another important
application is in the field of reproductive medicine, specifically in fertility treatments. (Trp6)-LHRH
can be used to optimize hormone levels in women undergoing assisted reproductive technologies like in
vitro fertilization (IVF). By controlling the timing of ovulation and synchronizing the development of
multiple ovarian follicles, (Trp6)-LHRH can improve the chances of harvesting mature eggs for
fertilization, thus potentially increasing the success rates of such fertility
programs.
Moreover, (Trp6)-LHRH analogs might also be considered for conditions like
endometriosis and uterine fibroids. Endometriosis is a painful disorder where tissue similar to the
lining inside the uterus grows outside the uterus. Uterine fibroids are benign tumors in the uterus that
can cause heavy menstrual bleeding and pelvic pain. In both scenarios, reducing estrogen levels via
(Trp6)-LHRH can help shrink existing fibroids and reduce the symptomatic suffering from endometriosis,
providing significant relief to patients.
Apart from these, (Trp6)-LHRH is also explored for its
potential to assist with issues like severe premenstrual syndrome (PMS) and premenstrual dysphoric
disorder (PMDD). For some women, the reduction in hormone fluctuations facilitated by (Trp6)-LHRH
treatment can alleviate the severe mood swings and depressive symptoms associated with these
conditions.
Overall, while (Trp6)-LHRH is prominently known for its applications in cancer
treatment, its utility extends into various non-cancerous medical fields. Always, when dealing with
non-cancerous conditions, treatment with (Trp6)-LHRH should be carefully monitored and customized to
each patient’s particular medical condition and therapeutic goals, ensuring the possible benefits
outweigh any adverse effects. Patients should always engage in thorough discussions with their
healthcare providers to fully understand the ramifications and expected outcomes of employing
(Trp6)-LHRH in managing their specific health issues.
How should (Trp6)-LHRH be administered for
optimal effects?
The administration of (Trp6)-LHRH for optimal therapeutic outcomes requires
careful consideration of dosing schedules, routes of administration, and patient monitoring. (Trp6)-LHRH
is usually administered by injection, which can be done either subcutaneously or intramuscularly,
depending on the specific formulation and treatment protocol. The frequency and dosage of administration
can vary widely depending on the specific medical condition being treated, the individual patient's
needs, and the specific (Trp6)-LHRH analog being used.
For conditions such as prostate cancer,
(Trp6)-LHRH is often administered as a long-acting depot injection, which can be given every one, three,
or six months. These formulations are designed to maintain a steady, sustained release of the hormone
analog over time, minimizing the need for frequent dosing and aiming for consistent suppression of
testosterone levels. This long-acting feature is beneficial as it can reduce the burden of frequent
clinic visits for patients and maintain adherence to the treatment regimen.
In contrast, for
fertility treatments or control of hormonal conditions like precocious puberty, the dosing may differ.
It could involve more frequent, perhaps even daily, subcutaneous injections to ensure precise control
over hormone levels and timing. In assisted reproductive technologies, for example, careful
synchronization with other hormonal treatments is essential for coordinating the development of ovarian
follicles.
Regardless of the condition being treated, achieving optimal effects with (Trp6)-LHRH
necessitates rigorous monitoring of hormone levels through blood tests. This monitoring helps ensure
that the desired suppression or simulation of hormonal activity is achieved and maintained
appropriately. Patients using (Trp6)-LHRH may undergo regular hormone level assessments to track
testosterone, estrogen, and related markers. This monitoring is crucial not just for ensuring efficacy
but also for reducing the risk of adverse effects related to over-suppression of reproductive
hormones.
Patient education is also a key component of effective (Trp6)-LHRH administration.
Healthcare providers typically educate patients on recognizing potential side effects early and
maintaining lifestyle choices that help manage them. They may include dietary adjustments to support
bone health and strategies to address hot flashes or mood changes.
In summary, the optimal
administration of (Trp6)-LHRH involves a comprehensive treatment plan personalized to the specific
health condition, closely monitored by healthcare professionals, and complemented by patient engagement
and education. These elements collectively contribute to maximizing the therapeutic benefits while
minimizing the risks associated with hormone modulation therapy.