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New Cryptophycins for ADC and SMDC

总结

New conjugation of cryptophycins for use in ADC (antibody-drug conjugates) and SMDC (small molecule drug conjugates)

技术优势

The present invention combines new synthetic ways to new Cryptophycin derivatives with alternative conjugation possibilites and pico-molar cytotoxicies, for ADC and SMDC synthesis. It can be linked to selective antibodies, peptides or other ligands which address tumour antigens and may therefore be used for anticancer therapy.

技术应用

To circumvent such side effects, cryptophycin could be used as payload for drug-conjugates. For treatment of solid tumours ADCs have only little effects, therefore SMDCs have more advantages in relation. To date, there are only few ADCs approved for cancer therapy and higher diversity is desirable to compensate for emerging resistances. In addition, there is also need in the art for novel, highly potent toxins, with no cryptophycin-based ADCs being approved so far.

详细技术说明

Cryptophycins are discussed as potential medicaments against cancer due to their high cytotoxic and cytostatic effect. They target tubulin and block the microtubule formation, leading to high cytotoxicity against many cancer cell lines. Moreover, as they are a weak target for the P-gp efflux pump, the cytotoxicity is only slightly reduced in multidrug-resistant (MDR) cancer cells. Due to these characteristics, several cryptophycin analogues were investigated as chemotherapeutics and cryptophycin-52 was even brought to the clinics. However, these were discontinued in phase II because of neurotoxic side effects and insufficient efficacy. These effects made a direct approach unusable for cancer treatment so far.

合作类型

Licensing

申请日期

19/02/2021 00:00:00

申请号码

EP 21 158 130.1

其他

No CN patents

ID号码

5817

国家/地区

德国