Corporate Banner
Satellite Banner
Scientific Community
Become a Member | Sign in
Home>News>This Article

4SC Reports Positive Data from Clinical Phase I trial with 4SC-205 in Cancer Patients

Published: Thursday, March 28, 2013
Last Updated: Wednesday, March 27, 2013
Bookmark and Share
All primary objectives of the clinical study achieved.

4SC AG has announced clinical data of the Phase I 'AEGIS' trial with the anti-cancer compound 4SC-205 in tumour patients. All primary study objectives were achieved. A comprehensive safety and tolerability profile of 4SC-205 was established.

As well as ascertaining the maximum tolerated dose (MTD) and dose limiting toxicities (DLTs), an excellent pharmacokinetic profile of the oral compound was established. In addition, the analysis of pharmacodynamic biomarkers demonstrated the intended mode of action.

The study data and new preclinical findings about the therapeutic target warrant further clinical evaluation of 4SC-205 in cancer patients. The Company, therefore, has decided on a study amendment, which will evaluate a new, adapted dosing scheme.

The first patient has now been treated according to the new scheme. 4SC-205 inhibits specifically the human kinesin spindle protein Eg5 which has been shown to play a crucial role in cell division (mitosis) and, therefore, in tumour growth.

To the Company's best knowledge, 4SC-205 is the only orally available Eg5 inhibitor in clinical development, worldwide.

Study design and positive results
The 'first-in-man', two-centre, dose-escalating Phase I study ('AEGIS' study) investigated safety, tolerability, pharmacokinetics, and pharmacodynamics of 4SC-205 in 46 patients with advanced solid tumours.

In two treatment cycles, each over three weeks, patients were treated with ascending oral doses of 4SC-205 in order to establish the MTD and potential DLTs.

Patients were treated in two different dose schedules: in the first dose schedule, patients received once-weekly dosing on days 1 and 8 of each cycle; in a second dose schedule patients received twice-weekly dosing on days 1, 4, 8 and 11 of each cycle.

In patients receiving once-weekly dosing, the MTD was established at the 150 mg dose level; in patients receiving a twice-weekly dosing, an MTD of 75 mg was established.

DLTs were reached at the treatment doses of 200 mg with once-weekly dosing and of 100 mg with twice-weekly dosing. Main side effects at DLT level were neutropenia and stomatitis of grade 3-4.

Moreover, 4SC-205 showed an excellent pharmacokinetic profile with a dose proportional increase of exposure and an elimination half-life of about 10 hours providing the basis for effective dosing schedules since the biological activity of the compound could be demonstrated via biomarker analysis of patients' skin biopsy samples.

Here, a dose dependent accumulation of cells arrested in cell division could be observed. Thus, 4SC-205 effectively exhibits the anticipated mode of action - inhibition of cell division (mitosis) - at clinically tolerated doses.

AEGIS study amendment
The clinical findings generated to date from this trial as well as new preclinical data about the therapeutic target and distribution of 4SC-205 in tissue, strongly support further clinical investigation of the compound applying an additional treatment schedule. The study has, therefore, been amended in order to investigate a new and innovative dosing scheme of 4SC-205 for the first time in cancer patients.

According to the amendment, another 9 to 12 eligible patients are expected to be enrolled in the trial. Following recent approval of the amendment by authorities, the first patient has now been treated. The results of the amended AEGIS study protocol are expected for mid 2013.

Dr Ulrich Dauer, Chief Executive Officer of 4SC, commented: 'We are pleased that in our AEGIS trial we have achieved all primary endpoints so far. 4SC-205 inhibits with high specificity an intriguingly interesting therapeutic target in anti-cancer treatment, the Eg5 protein, which plays a central role in cell mitosis and tumour growth. The encouraging biomarker response to 4SC-205 as shown in the study and new preclinical findings regarding the therapeutic target, make a strong case to further study our drug candidate in a new, highly innovative dosing scheme. This is expected to form a basis for the further evaluation of the compound in Phase II development. The fact that 4SC-205 is the only oral Eg5 inhibitor in clinical development is a strategic strength that facilitates the possibility to further explore alternative and enhanced dosing schemes.'

Further Information
Access to this exclusive content is for Technology Networks Premium members only.

Join Technology Networks Premium for free access to:

  • Exclusive articles
  • Presentations from international conferences
  • Over 2,700+ scientific posters on ePosters
  • More than 3,800+ scientific videos on LabTube
  • 35 community eNewsletters

Sign In

Forgotten your details? Click Here
If you are not a member you can join here

*Please note: By logging into you agree to accept the use of cookies. To find out more about the cookies we use and how to delete them, see our privacy policy.

Related Content

4SC AG Discuss "Epigenetic Regulation of Immunogenicity" at 10th Scientific Symposium
"Epigenetic therapy a vital component in the fight against cancer".
Saturday, October 10, 2015
4SC Receives Funding from the Eurostars Programme
Three-year research programme in cooperation with two other European epigenetics companies funded.
Saturday, October 03, 2015
4SC Strengthens Patent Protection for its Epigenetic Cancer Drug Candidate 4SC-202
A selective inhibitor of LSD1 and HDACs 1, 2, and 3 - in China.
Tuesday, August 18, 2015
4SC Strengthens Patent Protection for Lead Cancer Compound Resminostat
US patent for medical use in cancer and Canadian composition of matter patent granted.
Wednesday, July 01, 2015
4SC's Partner Yakult Honsha Starts Clinical Phase I Study in Pancreatic Tract Cancer Patients
Safety, tolerability and efficacy of resminostat in combination with S-1 chemotherapy will be investigated in various dosing schemes in order to determine dose regimen for potential subsequent Phase II trials in advanced pancreatic and/or biliary tract cancer.
Friday, June 26, 2015
4SC Signs Licensing and Development Agreement with Menarini
Licensing partnership for 4SC's cancer compound resminostat for the Asia-Pacific region excluding Japan.
Thursday, April 16, 2015
Prof. Dr. Helga Rübsamen-Schaeff and Joerg von Petrikowsky Join 4SC AG
Prof. Dr. Rübsamen-Schaeff and Mr. von Petrikowsky will replace the Supervisory Board members Dr. Thomas Werner and Klaus Kühn.
Saturday, January 17, 2015
4SC Reports Positive Topline Data from Clinical Phase I Trial with 4SC-205
4SC-205 is the only oral inhibitor of the Eg5 kinesin protein in clinical development worldwide. Eg5 plays a crucial role in cell division and tumour growth.
Friday, December 12, 2014
4SC Further Strengthens Patent Protection for its Lead Compound Resminostat
US Patent granted for the manufacturing process of resminostat.
Tuesday, October 21, 2014
4SC's Partner Yakult Honsha Completes Phase I Part of Clinical Study with Resminostat in NSCLC Patients
Phase I confirms safety and tolerability of resminostat/docetaxel combination in the planned dose regimen in Asian NSCLC patients.
Saturday, October 11, 2014
CRELUX and 4SC Discovery Awarded Research Grant
Project for identifying new bromodomain inhibitors initiated under the Munich m4 biotech cluster programme.
Thursday, July 24, 2014
4SC Hires Experienced Pharmaceutical Manager and Oncology Expert
Dr Erich Enghofer joins 4SC in the newly created position of Executive Vice President.
Friday, July 04, 2014
4SC Announces Positive Top Line Data from Clinical Phase I TOPAS Study
Company will present data from Phase I trial with epigenetic cancer drug 4SC-202 in patients with haematological tumours at ASCO.
Friday, May 30, 2014
4SC Presents Results from Analysis of Biomarkers in Phase II SHELTER Trial in HCC
Oral presentation of detailed results at ILCA conference, 15 Sept. 2013, Washington D.C.
Friday, September 13, 2013
4SC's Partner Yakult Honsha Starts Clinical Phase I/II Study with Resminostat in NSCLC
The Phase I/II study will investigate safety and efficacy of resminostat/docetaxel combination vs. docetaxel alone as a novel treatment option for patients with advanced, metastatic, or recurrent NSCLC.
Thursday, July 25, 2013
Scientific News
Removing 62 Barriers to Pig–to–Human Organ Transplant in One Fell Swoop
The largest number of simultaneous gene edits ever accomplished in the genome could help bridge the gap between organ transplant scarcity and the countless patients who need them.
Gene Editing Could Enable Pig-To-Human Organ Transplant
The largest number of simultaneous gene edits ever accomplished in the genome could help bridge the gap between organ transplant scarcity and the countless patients who need them.
Antioxidants Cause Malignant Melanoma to Metastasize Faster
Fresh research at Sahlgrenska Academy has found that antioxidants can double the rate of melanoma metastasis in mice.
UC San Diego Team Up with Illumina to Speed-Read Your Microbiome
Data analysis app accelerates studies aimed at using microbes to predict, diagnose and treat human diseases.
Paving the Way for Diamonds to Trace Early Cancers
Researchers from the University of Sydney reveal how nanoscale 'diamonds' can light up early-stage cancers in MRI scans.
Researchers Develop Classification Model for Cancers Caused by KRAS
Most frequently mutated cancer gene help oncologists choose more effective cancer therapies.
Chromosomal Chaos
Penn study forms basis for future precision medicine approaches for Sezary syndrome
Shaking Up the Foundations of Epigenetics
Researchers at the Centre for Genomic Regulation (CRG) and the University of Barcelona (UB) published a study that challenges some of the current beliefs about epigenetics.
Genetic Defences of Bacteria Don’t Aid Antibiotic Resistance
Genetic responses to the stresses caused by antibiotics don’t help bacteria to evolve a resistance to the medications, according to a new study by Oxford University researchers.
Tolerant Immune System Increases Cancer Risk
Researchers have found that individuals with high immunoCRIT ratios may have an increased risk of developing certain cancers.
Skyscraper Banner

Skyscraper Banner
Go to LabTube
Go to eposters
Access to the latest scientific news
Exclusive articles
Upload and share your posters on ePosters
Latest presentations and webinars
View a library of 1,800+ scientific and medical posters
2,700+ scientific and medical posters
A library of 2,500+ scientific videos on LabTube
3,800+ scientific videos