Oncology Pipeline

Remember to speak to your healthcare professional first if you have questions on any of our treatments in development.

Category

TINOSTAMUSTINE

The multi-action therapy, tinostamustine, is an alkylating deacetylase inhibiting molecule (AK-DACi) in development for a range of rare or difficult-to-treat blood cancers and solid tumours.

Tinostamustine is currently in Phase I clinical trials.

Rationale for development

Despite significant advances in cancer treatment, there are wide disparities in outcomes between different types of cancer and many patients have limited treatment options. Traditional DNA-damaging therapies have certain limitations which can result in resistance. These include, failure to gain access to the DNA strands to break them, or an inability to counteract DNA repair mechanisms within cancer cells.

Mechanism of action

Tinostamustine is a multi-action therapy, that is one that brings together multiple modes of action in the same treatment to offer new possibilities for patients with limited options.

In pre-clinical studies, tinostamustine has been shown to improve access to the DNA strands within cancer cells, break them and counteract damage repair.

Findings of pre-clinical studies

Pre-clinical studies with tinostamustine as monotherapy have shown significant response, with slowed disease progression in myeloid and lymphoid malignancies and solid tumours. When given in combination with agents such as bortezomib and dexamethasone, tinostamustine has been shown to act synergistically, offering the possibility of enhanced efficacy, improved duration of response, and improved depth of response. The administration of tinostamustine in novel combinations may provide physicians with additional approaches for the treatment of those patients with relapsed or refractory disease.

ETOPOSIDE TONIRIBATE

Etoposide toniribate is a tumour-activated therapy, in development for biliary tract cancer.

Plans for Phase III clinical trials are currently in development.

Rationale for development

Biliary tract cancer is the second most common primary hepatobiliary cancer, after hepatocellular cancer. It is estimated that almost 140,000 deaths occur each year from biliary tract cancer, a 22% increase since 1990. Surgery and chemotherapy are commonly used for early and locally advanced disease, however, there are no indicated second-line treatments.

Mechanism of action

Etoposide toniribate is hydrolysed at the site of the tumour by carboxylesterase, an enzyme overexpressed by some tumours, to produce activated etoposide. Activated etoposide binds to and inhibits topoisomerase II, which is often elevated in tumours, resulting in double strand breaks in tumour DNA. Once the tumour DNA has been damaged, this induces apoptosis.

Findings of clinical studies

In Phase II studies etoposide toniribate demonstrated efficacy in patients with advanced biliary tract cancers who had relapsed following treatment with the current standard of care. Overall, 56% of patients enrolled in the study met the primary study objective of disease control, including tumour shrinkages.

Etoposide toniribate is designated as an orphan drug for the treatment of biliary tract cancers for which there are no second-line treatment options.

EDO-B278

EDO-B278 is an antibody-drug conjugate targeting human tissue factor and is in development to treat various solid tumours.

EDO-B278 is currently in pre-clinical development, which means it is not yet being tested in humans.

EDO-B776

EDO-B776 is designed to target a fragment of cancer antigen 125 (CA125) and is being developed to treat ovarian cancer.

EDO-B776 is currently in pre-clinical development, which means it is not yet being tested in humans.

Rationale for development

Ovarian cancer represents an area of huge unmet medical need, with little progress made in terms of outcomes over the last few years. CA125 is shed from the tumour and circulates in the blood of individuals with ovarian cancer.

Mechanism of action:

EDO-B776 is designed to bind only to that fragment of CA125 that remains on the tumour surface after shedding so that the anti-cancer drug is delivered directly to the tumour.

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