Synonym |
Phe7-Afamelanotide |
Species |
Human |
Protein Accession |
P21333 |
Purity |
Greater than 95% as determined by RP-HPLC |
Endotoxin Level |
Less than 1 EU/μg as determined by LAL method |
Biological Activity |
The ED50 as determined by its ability to stimulate adenylate cyclase activity in HEK293 cells is
less than 0.1 nM |
Expression System |
E. coli |
Fusion Tag |
None |
Predicted Molecular Mass |
1648.9 Da |
Formulation |
Lyophilized from a 0.2 μm filtered solution of 20% acetonitrile and 0.1% TFA |
Reconstitution |
It is recommended to reconstitute the lyophilized Phe7-Afamelanotide in sterile 18 MΩ-cm H2O not
less than 100 μg/ml, which can then be further diluted to other aqueous solutions |
Storage & Stability |
Store lyophilized Phe7-Afamelanotide at -20°C. Aliquot the product after reconstitution to avoid
repeated freezing/thawing cycles. Reconstituted Phe7-Afamelanotide can be stored at 4°C for a
limited period of time; it does not show any change after two weeks at 4°C. |
FAQ
What is (Phe7)-Afamelanotide, and how does it work?
(Phe7)-Afamelanotide is a synthetic peptide
drug that mimics the effects of the naturally occurring hormone alpha-melanocyte-stimulating hormone
(α-MSH) in the body. This drug primarily functions to stimulate melanocytes, which are cells responsible
for producing melanin, the pigment that gives skin, hair, and eyes their color. As a potent analog of
α-MSH, (Phe7)-Afamelanotide binds to melanocortin receptors, primarily the MC1 receptor, on the surface
of the melanocytes. This binding triggers a cascade of reactions within the cells that lead to the
production of melanin, a process known as melanogenesis. The increase in melanin production results in a
darker skin tone, providing an enhanced photoprotective barrier against ultraviolet (UV) radiation from
the sun. By increasing skin pigmentation, (Phe7)-Afamelanotide offers potential protective effects
against sun-related damage, reducing the risk of UV-induced skin damage, sunburn, and potentially skin
cancer. This mechanism of action makes it particularly useful for individuals with conditions that cause
extreme sensitivity to sunlight, such as erythropoietic protoporphyria (EPP) and other photosensitivity
disorders. Additionally, the heightened melanin levels induced by (Phe7)-Afamelanotide can also provide
cosmetic benefits by offering those who have difficulty tanning naturally a way to achieve a more even
skin tone. However, it is essential to note that (Phe7)-Afamelanotide is primarily researched and
applied for medical purposes, especially in individuals who suffer from conditions with significant sun
sensitivity, rather than for purely aesthetic use. Its efficacy in increasing skin pigmentation and
protecting against photodamage makes it a promising therapeutic option for those dealing with these
specific conditions. The drug is administered via a subcutaneous implant, which gradually releases the
substance over time, ensuring a steady effect without the need for frequent dosing, thereby improving
patient compliance and the effectiveness of treatment.
What are the potential benefits of using
(Phe7)-Afamelanotide for people with photosensitivity disorders?
For individuals with
photosensitivity disorders, (Phe7)-Afamelanotide offers a groundbreaking therapeutic approach that
addresses the significant challenges posed by exposure to sunlight. One of the most notable benefits of
(Phe7)-Afamelanotide is its ability to enhance melanin production in the skin, providing an effective
natural barrier against ultraviolet (UV) radiation. This increased melanin level acts as a protective
shield, significantly reducing the risk of sunburn and other forms of sun-induced skin damage in
individuals who are extremely sensitive to sunlight. This therapeutic action is especially crucial for
individuals with erythropoietic protoporphyria (EPP), a genetic condition characterized by painful skin
reactions upon exposure to the sun. In such cases, (Phe7)-Afamelanotide has been shown to extend the
duration that these individuals can safely spend outdoors without experiencing adverse effects, thus
greatly improving their quality of life. Moreover, it enables greater participation in everyday
activities that were once limited by their condition. Beyond the immediate protective effects,
(Phe7)-Afamelanotide contributes to the psychological well-being of individuals with photosensitivity.
By mitigating the severity and frequency of painful skin reactions, patients experience less anxiety and
stress related to potential sun exposure. This emotional and mental health benefit adds a significant
layer to the overall quality of life improvements. Additionally, the drug's role in protecting against
longer-term consequences of sun exposure, such as increased risk of skin cancers, is a critical
consideration for those with long-standing exposure risks due to their condition. The sustained release
mechanism of (Phe7)-Afamelanotide through subcutaneous implantation ensures a constant level of the drug
in the system, providing consistent protection over extended periods. This method of administration
simplifies the treatment regimen, making it easier for patients to adhere to and achieve maximum
therapeutic benefit. Overall, (Phe7)-Afamelanotide represents a vital advancement in managing the
challenges associated with photosensitivity disorders, providing both physical and psychological relief
to individuals affected by these conditions.
What are the common side effects associated with
(Phe7)-Afamelanotide?
While (Phe7)-Afamelanotide offers significant benefits for individuals with
photosensitivity disorders, it is important to be aware of the potential side effects associated with
its use. Like any therapeutic drug, (Phe7)-Afamelanotide can have side effects, which vary in frequency
and intensity. The most commonly reported side effect is skin pigmentation changes beyond the intended
therapeutic effect, resulting in a darker shade than expected. This hyperpigmentation can sometimes
cause uneven skin tone, although it is generally reversible over time once the treatment is
discontinued. Another common side effect is erythema or redness at the site of the implant, which
typically resolves within a few days. Additionally, users may experience nausea, which is similar to the
response observed with other peptide-based drugs. Headaches are also a reported side effect linked to
(Phe7)-Afamelanotide usage. While these are usually mild, they can be bothersome for some individuals.
To manage this and other symptoms effectively, patients are encouraged to report any severe or
persistent side effects to their healthcare provider. Apart from these common reactions, some patients
may experience flu-like symptoms, including tiredness or general discomfort, shortly after receiving the
implant. These symptoms are typically transient, resolving as the body adjusts to the drug. It's
important to note that individual reactions to (Phe7)-Afamelanotide can vary, and while some individuals
may experience several side effects, others may have none. Healthcare providers will typically discuss
these potential issues with patients before starting treatment to ensure they are fully informed and
prepared to manage any adverse reactions. Although (Phe7)-Afamelanotide is considered safe and
well-tolerated, adherence to prescribed dosages and protocols is crucial in minimizing the risk of side
effects and ensuring optimal treatment outcomes. Regular follow-up appointments are advised to monitor
response and any emerging side effects, facilitating timely intervention if necessary. Overall,
understanding the potential side effects enables patients and healthcare providers to make informed
decisions about the use of (Phe7)-Afamelanotide in treating photosensitivity disorders.
How does
(Phe7)-Afamelanotide differ from traditional sun protection methods?
(Phe7)-Afamelanotide
represents a novel approach to sun protection that differs significantly from traditional methods such
as topical sunscreens, clothing, and shade-seeking behavior. Traditional sun protection methods
primarily work by creating a physical or chemical barrier on the skin's surface to reflect or absorb
ultraviolet (UV) rays, thereby reducing immediate exposure. Sunscreens, for instance, contain active
ingredients that either absorb UV radiation or reflect it, preventing it from penetrating the skin and
causing damage. However, these methods require consistent and proper application to be effective and can
be easily compromised by factors like sweating and swimming. Clothing and physical shade provide another
layer of protection but can be restrictive, limiting outdoor activities and comfort. In contrast,
(Phe7)-Afamelanotide works by stimulating the body’s own production of melanin, enhancing the skin’s
natural ability to protect against UV radiation. This endogenous increase in melanin not only provides a
more uniform and sustained level of protection but also does so from within, offering a significant
advantage over surface-level barriers. The increased melanin acts as a photoprotective agent, absorbing
UV radiation before it can cause harm to the deeper layers of the skin. Furthermore, as
(Phe7)-Afamelanotide is administered via a subcutaneous implant, it does not require the regular
reapplication that topical sunscreens do, making it a more convenient option for continuous protection.
Another critical difference is the potential long-term benefits associated with the use of
(Phe7)-Afamelanotide, especially for individuals with inherent photosensitivity. By reducing the
incidence of sunburns and other UV-induced skin damage, this treatment may lower the risk of long-term
effects such as skin cancers and photoaging. These potential long-term benefits highlight its role not
only as a protective measure but also as a preventive one in the broader context of dermatological
health. In summary, while traditional sun protection methods remain valuable and effective,
(Phe7)-Afamelanotide offers an innovative, systemic solution that enhances the skin’s natural defenses,
offering sustained, consistent protection that is particularly beneficial for those with
photosensitivity disorders.
Is (Phe7)-Afamelanotide suitable for everyone? What considerations
should be taken into account before using it?
While (Phe7)-Afamelanotide offers considerable
benefits, it may not be suitable for everyone, and several considerations must be evaluated before its
use. Primarily, (Phe7)-Afamelanotide is designed for individuals who suffer from photosensitivity
disorders, such as erythropoietic protoporphyria (EPP), and its use is generally recommended for those
diagnosed with such conditions. For these individuals, the therapeutic benefits clearly outweigh
potential risks, given the significant improvement in quality of life and reduction in sunlight
sensitivity. However, those without photosensitivity disorders should consult healthcare professionals
before considering its use, as it is not primarily intended for cosmetic purposes like tanning. Before
starting (Phe7)-Afamelanotide treatment, medical professionals will typically conduct a thorough health
assessment to ensure the patient is an appropriate candidate. This assessment will include a review of
the individual’s medical history, current health status, and any underlying conditions that may
influence the treatment’s safety and efficacy. Patients with specific medical conditions, such as
cardiovascular issues, kidney or liver disease, or a history of skin cancer, may not be ideal candidates
for (Phe7)-Afamelanotide due to potential risks and complications. Another critical consideration is
potential interactions with other medications. Patients must disclose all medications they are currently
taking to their healthcare provider to assess compatibility with (Phe7)-Afamelanotide. Certain drugs
could interact adversely, diminishing effectiveness or increasing the likelihood of side effects.
Additionally, the decision to use (Phe7)-Afamelanotide must consider lifestyle factors and patient
preferences. As the drug is administered via an implant, individuals need to be comfortable with this
method of delivery and the process involved in receiving and maintaining the implant. Moreover, because
(Phe7)-Afamelanotide leads to increased pigmentation, it is important for individuals to be informed
about and comfortable with potential changes in skin tone, which can vary in extent and reversibility
upon discontinuation. Finally, it is crucial for patients to have realistic expectations and thoroughly
understand the potential outcomes and side effects discussed with their healthcare provider. Engaging in
an open dialogue ensures informed decision-making and a clear understanding of the treatment’s role
within the context of their overall health management strategy.