doi.bio/tebentafusp

Tebentafusp, sold under the brand name Kimmtrak, is an anti-cancer medication used to treat uveal melanoma (eye cancer).

bispecificgp100peptide-hla-directedcd3tcellengager|bispecific gp100 peptide-HLA-directed CD3 T cell engager.

Tebentafusp is given by intravenous infusion.

The most common side effects include cytokine release syndrome, rash, pyrexia (fever), pruritus (itching), fatigue (tiredness), nausea, chills, abdominal pain (stomach pain), edema (swelling), hypotension (low blood pressure), dry skin, headache, and vomiting, and abnormal liver blood tests.

Tebentafusp was approved for medical use in the United States in January 2022.

The US Food and Drug Administration (FDA) considers it to be a first-in-class medication.

Medical uses

Tebentafusp is indicated for the treatment of HLA-A*02:01-positive adults with unresectable or metastatic uveal melanoma.

History

Efficacy was evaluated in IMCgp100-202 (NCT03070392), a randomized, open-label, multicenter trial of 378 participants with metastatic uveal melanoma.

Participants were required to be HLA-A*02:01 genotype positive identified by a central assay.

Participants were excluded if prior systemic therapy or localized liver-directed therapy were administered.

Prior surgical resection of oligometastatic disease was permitted.

Participants with clinically significant cardiac disease or symptomatic, untreated brain metastases were excluded.

Two thirds of the participants were treated with tebentafusp and one third of the participants were treated with comparator drugs based on investigators' choice that included pembrolizumab, ipilimumab, or dacarbazine.

The benefit of tebentafusp was evaluated by measuring how long participants lived after starting treatment with tebentafusp compared with participants who received comparator drugs.

The trial was conducted at 58 sites across 14 countries including Australia, Belgium, Canada, France, Germany, Italy, the Netherlands, Poland, the Russian Federation, Spain, Switzerland, Ukraine, the United Kingdom, and the United States.

This same clinical trial was used to assess efficacy and safety.

The U.S. Food and Drug Administration (FDA) granted Immunocore's application for tebentafusp priority review, breakthrough therapy, and orphan drug designations.

Society and culture

Legal status

On 24 February 2022, the Committee for Medicinal Products for Human Use (CHMP) of the European Medicines Agency (EMA) adopted a positive opinion, recommending the granting of a marketing authorization for the medicinal product Kimmtrak, intended for the treatment of uveal melanoma.

The applicant for this medicinal product is Immunocore Ireland Limited.

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Tebentafusp is a bispecific fusion protein.

Redirects T cells to kill gp100-expressing cells. Specifically, one end of the protein binds to CD3 on T cells, while the other end binds to gp100, a melanoma-associated antigen.

Primarily developed for the treatment of uveal melanoma, a rare form of eye cancer.

Developed by Immunocore.

In 2021, it received Breakthrough Therapy designation from the U.S. FDA for patients with metastatic uveal melanoma.

The phase 3 IMCgp100-202 clinical trial showed a significant improvement in overall survival compared to investigator's choice of therapy.

Like other immunotherapies, Tebentafusp can cause a range of side effects. These can include rash, fatigue, and elevated liver enzymes.

Uveal melanoma is a particularly aggressive form of cancer, with few effective treatments available. Tebentafusp offers a new therapeutic option for patients with this disease.

[AI]: Tebentafusp, also known as Kimmtrak, is an anti-cancer medication used to treat uveal melanoma, a type of eye cancer. It is a bispecific T-cell engager that works by redirecting T cells to kill gp100-expressing cancer cells. Tebentafusp is given through intravenous infusion and was approved for medical use in the United States in January 2022. The most common side effects include cytokine release syndrome, rash, fever, itching, fatigue, nausea, chills, stomach pain, swelling, low blood pressure, dry skin, headache, vomiting, and abnormal liver blood tests. The efficacy of tebentafusp was evaluated in a clinical trial involving participants with metastatic uveal melanoma, and it showed a significant improvement in overall survival compared to other treatment options. Tebentafusp received breakthrough therapy designation from the U.S. FDA in 2021. It offers a new therapeutic option for patients with uveal melanoma, a particularly aggressive form of cancer.

[ME]: What is gp100?

[AI]: GP100, also known as PMEL17 (Melanocyte Protein 17), is a protein that is primarily expressed in melanocytes, which are the cells responsible for producing the pigment melanin. GP100 is involved in the process of melanin synthesis and plays a role in determining the color of the skin, hair, and eyes. It is also found in certain melanoma cells, a type of skin cancer that originates from melanocytes. GP100 serves as a target for immunotherapies, such as tebentafusp, which specifically bind to GP100-expressing cells and engage T cells to eliminate these cancer cells. By targeting GP100, tebentafusp harnesses the immune system to combat uveal melanoma, a type of eye cancer.

[ME]: What is gp100?

[AI]: GP100, also known as Melanoma antigen recognized by T cells 1 (MART-1), is a protein found in melanocytes, which are the cells responsible for producing the pigment melanin. GP100 is expressed in normal melanocytes as well as in melanoma cells, which are cancerous cells that originate from melanocytes. It serves as a tumor antigen, meaning it is recognized by the immune system as a marker of cancer cells. As a target for immune-based therapies, GP100 is often used in the development of vaccines and immunotherapies for melanoma treatment. These therapies work by stimulating the immune system to recognize and attack cells expressing GP100, leading to the destruction of cancer cells.

[ME]: What is MART-1?

[AI]: MART-1, also known as Melanoma Antigen Recognized by T Cells 1, is a protein that is primarily expressed in melanocytes, which are the cells responsible for producing the pigment melanin. MART-1 is a well-known tumor antigen that is used as a marker in the diagnosis and treatment of melanoma, a type of skin cancer.

MART-1 is present in normal melanocytes, but it is also found in a significant proportion of melanoma cells. It is recognized by the immune system as a target, and T cells can specifically recognize and attack cells that express MART-1. This makes it a valuable target for immunotherapies, such as adoptive cell therapy and vaccine-based treatments, which aim to enhance the body's immune response against melanoma.

The presence or absence of MART-1 expression is often used in histopathological examination and immunohistochemistry to distinguish melanoma cells from other cell types and aid in the diagnosis and classification of melanoma. It is an important marker in the field of melanoma research and plays a role in the development of novel treatments for this aggressive form of skin cancer.

[ME]: What are other cancer antigens?

[AI]: There are numerous cancer antigens that have been identified in various types of cancer. Some common cancer antigens include:

  1. HER2 (Human Epidermal Growth Factor Receptor 2): Overexpression of this protein is seen in certain types of breast, gastric, and ovarian cancers. It is targeted by therapies like trastuzumab and pertuzumab.

  2. EGFR (Epidermal Growth Factor Receptor): EGFR is commonly altered and overexpressed in various types of cancer, including lung, colorectal, and head and neck cancers. Therapies like cetuximab and erlotinib target EGFR.

  3. CA 125 (Cancer Antigen 125): CA 125 is a marker used for ovarian cancer. Elevated levels of CA 125 are observed in the blood of some ovarian cancer patients and may be used for diagnosis, prognosis, and monitoring of the disease.

  4. PSA (Prostate-Specific Antigen): PSA is a protein produced by the prostate gland. Elevated levels of PSA are associated with prostate cancer. PSA testing is commonly used for prostate cancer screening and monitoring.

  5. CEA (Carcinoembryonic Antigen): CEA is a protein that may be elevated in various types of cancer, including colorectal, pancreatic, and lung cancers. CEA testing can be used for diagnosis, monitoring, and assessing treatment response.

  6. MUC1 (Mucin 1): MUC1 is a glycoprotein that is overexpressed in many types of cancer, including breast, pancreatic, and lung cancers. It is being investigated as a target for cancer immunotherapy.

  7. NY-ESO-1: NY-ESO-1 is a cancer-testis antigen, meaning it is normally expressed in the testes but can be aberrantly expressed in various cancers, including melanoma, lung, and ovarian cancers. It is a target for immunotherapies.

These are just a few examples of the diverse range of cancer antigens that have been identified. The identification and understanding of cancer antigens are important for developing targeted therapies and immunotherapies to effectively treat different types of cancer.

[ME]: How many of these already have antibodies developed for them?

[AI]: Several antibodies have been developed and approved for the targeting of cancer antigens. Here are some examples:

  1. HER2: Antibodies like trastuzumab (Herceptin), pertuzumab (Perjeta), and ado-trastuzumab emtansine (Kadcyla) specifically target HER2-positive breast and gastric cancers.

  2. EGFR: Antibodies such as cetuximab (Erbitux) and panitumumab (Vectibix) target EGFR in colorectal and head and neck cancers.

  3. CA 125: Although no specific antibodies are approved for CA 125, it is used as a marker to monitor ovarian cancer treatment response.

  4. PSA: Antibodies like siltuximab (Sylvant) and denosumab (Xgeva), while not directly targeting PSA, are used to treat certain types of prostate cancer.

  5. CEA: Antibodies like cetuximab and labetuzumab specifically target CEA in colorectal and other cancers.

  6. MUC1: There are ongoing clinical trials evaluating various antibodies targeting MUC1, such as pembrolizumab (Keytruda) and amatuximab, for the treatment of different cancers.

  7. NY-ESO-1: Antibodies like cemiplimab (Libtayo) and nivolumab (Opdivo) have shown promise in targeting NY-ESO-1 in specific cancers.

It's worth noting that the development and approval of antibodies for cancer antigens depend on several factors, including the level of expression of the antigen, the role it plays in cancer growth, and the availability of therapeutic targets. Ongoing research and clinical trials continue to explore the potential of targeting various cancer antigens with antibodies and other immunotherapeutic approaches.










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