Synonym |
Antide, Iturelix, ORF 23541 |
Species |
Human |
Protein Accession |
P30968 |
Purity |
Greater than 95% |
Endotoxin Level |
Less than 1 EU/μg |
Biological Activity |
Not specified |
Expression System |
E. coli |
Fusion Tag |
None |
Predicted Molecular Mass |
About 2.7 kDa |
Formulation |
Lyophilized from a 0.2 μm filtered solution in Acetonitrile and TFA |
Reconstitution |
Reconstitute in distilled water at a concentration of 0.1 mg/ml |
Storage & Stability |
Store at -20°C. Stable for up to 12 months from date of receipt |
FAQ
What is Antide, and how does it work?
Antide is a synthetic peptide drug primarily used in the
field of endocrinology as a GnRH (Gonadotropin-releasing hormone) antagonist. It plays a pivotal role in
regulating the hormonal environment, particularly by suppressing the release of gonadotropins from the
pituitary gland. This action makes Antide efficient in controlling reproductive function and has
potential therapeutic applications in various medical conditions that require the downregulation of
certain hormones. The mechanism of action of Antide involves binding to GnRH receptors in the pituitary
gland with high affinity. By doing so, it prevents the natural GnRH produced by the hypothalamus from
interacting with these receptors. This blockade results in a decrease in the release of two crucial
hormones: follicle-stimulating hormone (FSH) and luteinizing hormone (LH). These hormones play
significant roles in reproduction, primarily by influencing the function of the ovaries and testes. In
clinical and research settings, the ability of Antide to modulate the reproductive hormonal axis without
the inherent agonistic effects of GnRH analogs offers a more immediate suppression of gonadotropins
compared to traditional GnRH agonists, which initially create a surge in hormone levels before
downregulating them. This makes Antide particularly useful in situations where quick suppression of
hormone levels is desired, such as in certain cancer treatments. Potential applications of Antide extend
beyond just reproductive health. It can be instrumental in addressing hormone-sensitive cancers, such as
prostate cancer in men and breast cancer in women. By significantly reducing LH and, consequently,
testosterone levels in men, and similar pathways in women, it reduces the stimulatory effects of these
hormones on cancer growth. The ability to finely tune the body's hormonal milieu without inducing the
initial surge seen with other treatments marks Antide as a significant advancement in medical science.
Importantly, while Antide provides numerous benefits, potential side effects and risks need to be
considered, which requires close supervision by a healthcare professional.
How does Iturelix
differ from other GnRH antagonists?
Iturelix is a notable GnRH antagonist that stands out due to
its distinct structure and pharmacological profile compared to other GnRH antagonists. This
differentiation primarily lies in its biochemical structure, metabolic stability, and the specific
receptor binding affinity that underscore its applications and benefits. Typically, GnRH antagonists
function by directly inhibiting the GnRH receptors in the pituitary gland, which in turn reduces the
release of key hormones like LH and FSH. Iturelix is engineered to have a unique conformation that not
only enhances its selective binding to these receptors but also improves its pharmacokinetic profile.
This selectivity ensures that the drug has a precise action, minimizing potential off-target effects
that could lead to undesirable side effects. Structurally, Iturelix features modifications that resist
enzymatic degradation, which enhances its metabolic stability. This means that Iturelix can remain
active in the body for a longer period compared to some of its counterparts, thus ensuring a more
sustained receptor antagonism. Such a feature could potentially lead to less frequent dosing, which is
an advantageous benefit for patients requiring GnRH antagonist therapy over extended periods.
Furthermore, the reduced risk of degradation ensures that the compound remains effective throughout its
duration of action, leading to better therapeutic outcomes. Unlike traditional GnRH antagonists,
Iturelix may also exhibit differential affinity for various receptor subtypes, which could be exploited
for more tailored therapeutic applications. This characteristic allows it to be more versatile in
treatment options, potentially opening new avenues in managing hormonal imbalances and related
disorders. Despite these advantages, like other drugs in its class, Iturelix must be used under strict
medical supervision to monitor any adverse effects or potential interactions with other medications. The
advancements in Iturelix's structure and function exemplify the ongoing efforts in pharmaceutical
science to develop more effective, safe, and patient-friendly treatment options.
What therapeutic
applications does ORF 23541 have?
ORF 23541 is a compound characterized by its potent GnRH
antagonistic properties and is being explored for a range of therapeutic applications. Its primary role
is to inhibit gonadotropin release, offering a potentially significant impact across various medical
domains, particularly where the modulation of sex hormones is beneficial. One of the noteworthy
applications of ORF 23541 is in the management of hormone-dependent cancers, including prostate cancer
in men and certain forms of breast cancer in women. By effectively lowering levels of circulating
testosterone and estrogen, ORF 23541 can help slow down or halt the progression of these cancers,
providing an adjunct or alternative to traditional treatments like chemotherapy, radiation, and surgical
interventions. This pharmacological action helps in potentially reducing tumor growth and improving
patient outcomes. Additionally, ORF 23541 finds potential use in reproductive medicine, particularly in
assisted reproductive technology (ART). By controlling the hormonal environment, it aids in preventing
premature ovulation, thereby enhancing the success rates of in vitro fertilization (IVF) procedures.
This is critical in creating a controlled ovarian stimulation environment which is crucial for
optimizing egg retrieval in ART cycles. Moreover, the compound's application extends into the arena of
gynecological disorders. By modulating gonadotropin levels, ORF 23541 may offer therapeutic benefits in
conditions characterized by excessive hormonal activity, such as polycystic ovary syndrome (PCOS) or
endometriosis, by reducing the impact of estrogen-driven symptoms and associated pathology. Furthermore,
the drug could potentially be leveraged in male contraceptive therapies. By reducing testosterone
levels, ORF 23541 could act as an effective means of temporary and reversible contraception for men,
achieving a significant reduction in sperm production without the long-term impacts associated with
hormonal imbalances. Nevertheless, it's important to remember that as ORF 23541 is still under
investigation, its safety, efficacy, and optimal therapeutic regimens continue to be the focus of
rigorous clinical research and trials.
What are the potential side effects and risks associated
with Antide, Iturelix, and ORF 23541?
The use of Antide, Iturelix, and ORF 23541, as with any
pharmacological intervention, carries potential side effects and risks that must be carefully considered
and monitored. While these medications represent innovative strides in GnRH antagonist therapy,
understanding their side effect profiles is crucial for optimizing patient outcomes and safety. Common
to this class of drugs, patients may experience symptoms related to hormonal suppression, such as hot
flashes, headaches, and injection site reactions, when administered via the parenteral route. These are
generally mild and transient but can lead to patient discomfort, necessitating management strategies to
mitigate these experiences. The hormonal changes induced can lead to more significant implications. For
instance, long-term suppression of gonadotropins may result in alterations in bone mineral density,
escalating the risk of osteoporosis or fractures, particularly in populations already predisposed to
these conditions, such as postmenopausal women or older men. This requires diligent monitoring of
patients, with potential implementation of supplementary treatments like calcium or vitamin D to offset
such risks. Another important consideration is the potential impact of these drugs on cardiovascular
health. Reductions in sex steroids like testosterone and estrogen can influence lipid profiles and
vascular function, potentially increasing the risk of cardiovascular events, especially in individuals
with pre-existing cardiovascular conditions. Regular cardiovascular assessments and monitoring of lipid
levels might be necessary to circumvent these risks. Risk of hypersensitivity reactions, although rare,
can occur and necessitates immediate medical attention. These reactions may range from mild skin rashes
to more severe anaphylactic responses. It's paramount for healthcare professionals to evaluate patient
histories comprehensively to prevent such adverse outcomes. The risk-benefit ratio should be closely
examined in all cases, emphasizing patient education about possible side effects, and encouraging them
to report any unusual symptoms promptly. Regular follow-ups and dose adjustments based on therapeutic
response and tolerance levels help in maintaining the balance between efficacy and safety for each
patient. Ultimately, while these GnRH antagonists offer significant therapeutic promise, their use
demands a tailored approach underpinned by a thorough understanding of the individual patient's health
status, existing conditions, and concurrent medications.
How do Antide, Iturelix, and ORF 23541
contribute to advancements in cancer treatment?
Antide, Iturelix, and ORF 23541 are part of a
novel class of GnRH antagonists that have made substantial contributions to advancements in cancer
treatment, particularly hormone-dependent cancers. Their unique mechanism of action, which involves the
direct inhibition of GnRH receptors, provides a more targeted suppression of tumor-promoting hormones
such as testosterone and estrogen. This precise control over the hormonal milieu offers several
advantages over traditional therapies. In the context of prostate cancer, which thrives on androgens
like testosterone, these GnRH antagonists effectively lower circulating testosterone levels more rapidly
than GnRH agonists. With agonists, there is a known initial surge in hormones before suppression, which
can temporarily exacerbate cancer growth and lead to clinical flare-ups. In contrast, antagonists like
Antide and Iturelix provide immediate inhibition of testosterone without the surge, thus minimizing the
risk of stimulating cancer growth during treatment initiation. This immediate action can be crucial for
high-risk patients who require swift intervention. In treating breast cancer, particularly estrogen
receptor-positive types, these antagonists similarly lower estrogen levels, slowing disease progression.
They offer an important line of defense, especially for patients unresponsive to other hormone
therapies. Their ability to modulate estrogen levels presents a less invasive alternative to surgical
options like oophorectomy or radiation therapy aimed at reducing estrogen production. ORF 23541 and
related compounds further epitomize the potential for tailoring cancer therapies to an individual's
needs, promoting personalized medicine. The promising results of ongoing research into their use in
combination with other chemotherapies or targeted agents could enhance efficacy by addressing multiple
growth pathways simultaneously. Furthermore, their use can improve the quality of life for patients by
reducing the side effects associated with other cancer therapies. Unlike chemotherapy, which broadly
attacks dividing cells and causes significant side effects such as nausea, hair loss, and immune
suppression, GnRH antagonists provide a more focused approach that preserves non-target cells and
tissues. Additionally, this class of drugs may hold potential in preventing cancer recurrence by
maintaining low hormone levels, continuing to suppress tumor growth even in a residual state. The
continued development and research of Antide, Iturelix, and ORF 23541 in clinical trials indicates a
robust potential for these drugs not only to improve current treatment regimens but also to expand
therapeutic options for patients. In conclusion, these compounds embody a pivotal evolution in cancer
therapy, one driven by a deeper understanding of hormone pathways and the pursuit of safer, more
effective cancer treatments.