Antibody Drug Conjugate (ADC) Assets
ADC assets, developed by Iksuda Therapeutics.
Creating next-generation class leading ADCs for hard-to-treat cancers
Collaboration Programs
PermaLink® Proprietary conjugation chemistry for the creation of stable, differentiated ADCs.
Antibody Drug Conjugates (ADCs) represent a powerful addition to cancer treatment, with a mechanism that permits the delivery of potent cytotoxic agents directly to cancer cells using monoclonal antibodies that target tumour-specific antigens.
This selective approach to delivery of tumour killing payloads results in superior efficacy and fewer side effects for patients. Currently, there are over 80 ADCs in the clinic, comprised of a selection of payload classes, numerous linkers and a wide range of antibodies, directed towards many distinct antigens.
Stable conjugation is fundamental to ADC design and improving therapeutic index. The foundation of Iksuda’s ADCs is its proprietary conjugation chemistry PermaLink, which is associated with industry-leading conjugation stability.
PermaLink is a cysteine-specific, vinyl pyridine-based chemistry that demonstrates inherent conjugation stability and, unlike many other approaches to conjugation, Iksuda’s PermaLink chemistry is not susceptible to drug de-conjugation.
In Preclinical studies, PermaLink based ADCs are associated with improved tolerability and overall tumour response. The enhanced stability profile of PermaLink enables the safer use of ultra-potent payloads which, when conjugated to antibodies that are directed to well-selected targets, results in more efficacious ADCs.
PermaLink is available for collaboration research and license for the development of novel ADCs to nominated target antigens. For more information, please complete a request using the Contacts form or contact Dave or Ian at www.iksuda.com
Ultra-potency payloads
PermaLink enables the use of ultra-potent payloads in the design and development of effective ADCs. Iksuda has access to several payload series from known and novel drug classes, each with distinct mechanism of action but all able to potently induce apoptosis of cancer cells.
Iksuda’s focus is on DNA-interactive mechanisms.
DNA disruption is a well-known approach for anti-cancer drug development in general, as well as for ADC consideration. The current ADC clinical pipeline includes various DNA modifying payloads for which mechanisms include DNA cleavage, DNA intercalation (e.g. anthracyclines), DNA alkylation (duocarmycins and IGNs), DNA relegation inhibition (doxorubicin), double strand breaks (calicheamycins) and cross-linking (PBDs).
Iksuda is developing proprietary, next generation, ultra-potent DNA-disruptive payloads. For more information and discussions over the use of these payloads in collaborative ADC creation programmes, fill out the Contacts form or contact Ian or Dave directly
PermaLink-conjugated ADCs
IKS01: in preclinical development for the treatment of ovarian and lung cancer populations.
IKS01 targets the folate receptor and has shown significant anti-tumour efficacy in pre-clinical models of ovarian and lung tumours, each of which included a broad range of folate-receptor alpha (FRA) expression.
Frequent over-expression of FRA in ovarian and non-small-cell lung cancer (accounting for 80% of lung cancer cases) and relative lack of expression in normal tissue make it an attractive therapeutic target. However, anti-tumour activity is generally limited to patients whose tumours express high levels of FRA.
IKS01 is comprised of an FRA-targeting antibody conjugated via Iksuda’s PermaLink technology to Femtogenix’s highly potent FGX2-62 DNA minor groove binding payload. IKS01 is target specific and induces tumour regression in FRA-expressing models at doses that are well-tolerated. IKS01 treatment is associated with complete regression in low, moderate and high FRA-expressing models, with levels of efficacy that are significantly above benchmark ADCs.