From Japan, it is reported that scientists have managed to synthesize 11.5 grams of the halichondrin molecule with the E7130 index. This is an unprecedented event that the world has been waiting for for over 30 years. Until now, no one has managed to get more than a milligram of this unique substance, which put an end to all attempts to begin clinical trials of a potentially revolutionary drug. But now medicine is opening a new era.
Back in 1986, Japanese scientists isolated a new substance called polyester macrolide from Halichondria okadai sea sponge. Its molecules are called "halichondrin" (Halichondrin) and the first tests on animals showed that they are incredibly active in the fight against cancer cells. Everyone was eager to start creating a drug, but it quickly became clear that the structure of this molecule is extremely complex and cannot be synthesized.
Only in 1992 was it possible to obtain a very simplified version of halichondrin, a molecule called eribulin. And she very quickly found application in the treatment of breast cancer. Then another fifteen years passed before scientists from Harvard University and Japanese pharmacists from Eisai joined forces to solve the problem of halichondrin synthesis. They were helped by the developments of Professor Yoshito Kishi in the field of convergent synthesis methods - for the first time it was about the possibility of obtaining not milligrams, but whole grams of a substance.
And now, a miracle happened, as pharmacists say, because previously no one could have thought of a portion of halichondrin weighing more than 10 grams. This tricky molecule has 31 chiral centers, and the researchers propose that there are about 4 billion different wrong ways of orienting this molecule. But the main difficulties seem to be behind and the E7130 is now being prepared for the first clinical trials.