WILEX AG - Pipeline

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Clinical Programme

RENCAREX® (WX-G250)

Compound Class	Chimeric monoclonal antibody
INN (International Nonproprietary Name)	girentuximab
Indication	Clear cell renal cell cancer (ccRCC) and other solid tumours
Target	The Antibody WX-G250 binds specifically to the protein structure carbonic anhydrase IX (also called CA IX, MN or G250 antigen). CA IX is expressed on the cell surface of clear cell renal cell carcinomas but not on healthy renal tissue. The protein is also present in a variety of other solid tumours, e.g. bladder- and colon cancer.
Mode of Action	ADCC*
Development Status	Non-metastatic clear cell RCC, adjuvant therapy A pivotal Phase III trial with RENCAREX® as adjuvant therapy of patients with non-metastatic clear cell RCC at high risk of relapse after surgery has completed patient recruitment. Metastatic clear cell RCC, combination therapy with cytokines RENCAREX® has completed clinical Phase II trials in combination therapy with cytokines (IL-2 and IFN) in patients with metastatic RCC.
Orphan Drug Status	Orphan Drug Status for the U.S. and the EU in the indication RCC.
Partner	WILEX has granted Laboratorios del Dr. Esteve S.A. the commercialisation rights on RENCAREX® in certain countries of South Europe including Spain, Italy, Portugal, Andorra and Greece.
Development Rationale	Standard therapy for non-metastatic clear cell RCC is resection of the affected kidney and any associated tumour mass followed by observation. There is no adjuvant treatment approved by the FDA or EMEA for patients after surgery, although there is a high relapse rate among patients after surgery. RENCAREX® has proven to be safe and well-tolerated and is therefore ideally suited for this area of high medical need.
Background information	Please click here for further information on the RENCAREX® programme.

* Antibody-dependent cellular cytotoxicity ("ADCC") is the mechanism by which antibodies induce natural killer ("NK") cells or other effector cells of the patient’s immune system to destroy tumour cells.

** FDA: Food and Drug Administration, EMEA: European Medicines Evaluations Agency

REDECTANE®

Compound Class	Iodine-124 radiolabelled antibody
INN (International Nonproprietary Name)	iodine (124I) girentuximab
Indication	Kidney tumours
Target	The monoclonal antibody cG250 binds specifically to a protein structure on the cell surface of malignant tumour cells. This protein structure, called Carbonic anhydrase IX (also CA-IX, MN or G250 antigen) is found on over 90 % of clear cell renal cell carcinomas, but not on normal renal tissue.
Mode of Action	Diagnosis of malignant kidney tumours by means of PET/CT: As the antibody is radiolabelled malignant tumours can be visualised by means of positron emission tomography (PET). In combination with CT the accumulation in the tumour tissue can be localised.
Development Status	Phase III registration trial, FDA issued Special Protocol Assessment (SPA) in February 2008; patient recruitment was completed by the end of August 2009.
Development Rationale	REDECTANE® may be used before surgery to detect clear cell renal cancer in patients with renal masses. At present, only histopathology results after surgery can determine whether the tumour is benign or malignant. As clear cell renal cancers are associated with an aggressive phenotype their a priori determination may help guide appropriate surgical/therapeutic management.
Background information	Please click here for further information on the REDECTANE® programme. The Company´s cooperation partner, the Ludwig Institute for Cancer Research, New York carried out a proof-of-concept trial in cooperation with the Memorial Sloane-Kettering Cancer Center, New York. This feasibility study found that a positive result with REDECTANE® was confirmed as clear cell renal cell carcinoma in 100% of cases (positive predictive value).

MESUPRON®*

Compound Class	Oral small molecule serine protease inhibitor
Indications	Currently pancreatic and breast cancer, additional indications including ovarian and colon cancer possible
Target	Urokinase Plasminogen Activator (uPA) system WX-UK1 targets uPA and other serine proteases, which play a key role in tumour metastasis.
Mode of Action	Anti-metastatic, non-cytotoxic agent
Development Status	MESUPRON is an orally available pro-drug of WX-UK1. In preclinical studies, WX-UK1 has shown to effectively block metastasis formation and to reduce primary tumour growth. WX-UK1 Phase Ia trial: healthy volunteers, multi-dose study (monotherapy) Phase I/IIa trial: patients with sold tumours (monotherapy) Phase Ib trial: patients with head and neck cancer (monotherapy) Phase I trial: patients with metastatic breast cancer and other advanced solid tumours (combination therapy with Capecitabine) MESUPRON: Phase I trial: healthy volunteers (monotherapy) Phase I trial: healthy volunteers, dose escalation study (monotherapy) Phase I trial: patients with malignant head&neck cancers, dose escalation study (monotherapy) The substance was safe and well tolerated in all studies. Currently the following trials are being conducted: Phase II trial: patients with non-metastatic pancreatic cancer (combination therapy with gemcitabine) Phase II trial: patients with metastatic breast cancer (combination therapy with capecitabine)
Development Rationale	Oral MESUPRON® is being developed for the chronic treatment of patients with aggressive metastasising solid tumours.
Background Information	Please click here for further information on the uPA-programme.

WX-554

Compound Class	Orally available small molecule MEK inhibitor
Indication	Various cancers
Target	mitogen-activated protein kinase (MEK)
Mode of Action	The mitogen-activated protein kinase (MEK) has been shown to play a central role in signal transduction. MEK has been linked to a multitude of biological processes such as cell division, cell differentation and cell death. The MEK signalling pathway is overexpressend in more than 30 % of cancers, resulting in uncontrolled cell growth and proliferation. Inhibition of MEK could have significant therapeutic potential.
Development Status	The MEK inhibitor is currently in preclinical development. In August 2009, WILEX filed an application with the German Federal Institute for Drugs and Medical Devices (BfArM) for the approval of a Phase I trial. Approval has been granted in the meantime.
Background Information	Please click here for further information on the WX-554 programme.

WX-037

Compound Class	Small molecule PI3K inhibitor
Indication	Solid tumours, various cancers
Target	phosphatidylinositol-3-kinase/proteine-kinase (PI3K)
Mode of Action	The phosphatidylinositol-3-kinase/proteine-kinase-B signalling pathway – PI3K in short – sends a “growth” signal to the nucleus of a tumours cell. It has been shown that abnormal mutations of the PI3K signalling pathway are present in most types of cancer. Identifying an inhibitor for the PI3K signalling pathway is thus of therapeutic interest.
Development Status	The drug candidate WX-037 was selected as the lead compound for the oral small-molecule PI3K inhibitor, and a development plan has been prepared.
Background Information	Please click here for further information on the WX-037 programme.