Pipeline & Programs

Original and efficient candidates with proof of concept

CarboMimetics brings an original and efficient solution through its total synthesis expertise.

Two first drug candidates have already been identified in CarboMimetics oncology related programs.

pipeline&program

 

puce1CM20201, new generation of effective and neutralizable anticoagulant (potential Best-In Class)

Currently in the preclinical phase, CM20201, an efficient small glyco-drug with selective activity inhibition of Factor Xa, would be used in a first place for oncology related Deep Vein Thrombosis (DVT). Today, anticoagulants are the reference treatment but display major risk of uncontrollable life threatening bleeding. Thus, CM20201 displays significative advantages compared to the usual standard anticoagulants on market:

  • High anticoagulant activity demonstrated in animal model (Wessler model)
  • Further features as required by market unmet needs:
  • orally available,
  • no constant monitoring required
  • antidotable (total neutralization with avidin demonstrated in animal models)

Several heparin derivative drugs on market are not efficient enough as they still need monitoring control, have uncomfortable mode of administration (IP and Sc) and no antidotable.

Recently, new antidotes have been tested on clinical trial in combination with standard anticoagulants in order to reduce the hemorrhagy side effects. Nevertheless, these antidotes are not specific to a particular anticoagulant as its acts as a Factor Xa inhibitor, may play competition with anticoagulant itself and implies to be tested as an additional compound.

CM20201 overcomes this concern because it has the main advantage to be a fully synthetic heparin derivative conjugated to biotin. The efficient anticoagulant could thus be totally neutralized with Avidin and this complex is then rapidly eliminated. Besides, Biotin – Avidin neutralizing approach has already and successfully been tested in Phase III clinical trials with Idrabiotaparinux showing the high beneficial activity of CM20201 in DVT treatment.

 

puce2CM30119, lead candidate to reduce metastasis risk (potential First-In Class)

CM30119 targets an unexploited oncogenic and promising enzyme: Heparanase. This enzyme is overexpressed during disease development and correlated with tumor size/growth and vascularization, and metastases. During radiotherapy known to promote metastasis and to be inefficient by the time, Heparanase inhibition results in the increase of radiotherapy efficiency.

Currently in the lead optimization phase, CM30119, an efficient small glyco-drug, would be used in a first place as a therapeutic adjuvant for radiotherapy to increase the effectiveness of radiotherapy and reduce risk of metastasis for head and neck cancer patients. CM30119 already exhibits promising results with anti-angiogenesis and anti-metastatic therapeutic property.

Only few sugar related compounds targeting heparanase enzyme are currently under development for several cancers but some of them display serious hemorrhagic side effects because of their anticoagulant activity.

CM30119 provides real therapeutic properties:

  • Higher efficacy than competitive drugs demonstrated through in vivo studies
  • Better Drug Like properties
  • Higher and only selectivity for Heparanase
  • No anti-coagulant activity
  • Four CM30119 derivatives, potent heparanase inhibitors, already available to be evaluated in animal models

 

puce3 In addition to these drug candidates, CarboMimetics reinforces its portfolio with compounds targeting inflammation and diabetes:

  • CM30115, small glyco-drug, deeply inhibits chemokine RANTES induced THP1 cell migration
  • CM30139 and CM30143 increases glucose uptake in standard and insulin conditions on both adipocyte (3T3-L1) and muscle (H2K and L6) cell cultures.