In 2022, the market for colorectal cancer is valued at USD 18 billion, and it
is predicted to reach USD 24 billion by 2028. About 30-40% of patients wh
o undergo colorectal cancer treatment experience recurrence within 2-3 y
ears, and the care and survival rate after recurrence are difficult, with limit
ed effectiveness from traditional treatment. Our team has developed a sm
all molecule drug conjugation (Compound 10) that has been proven stabl
e in human plasma (with a half-life of approximately 36 hours) through in
vitro experiments. In a tumor microenvironment simulation of a proteolyti
c solution, Compound 10 effectively releases more than 90% of the active
drug SN38. In mice orthopedic experiments, we selected a more rigorous i
n situ cancer induction model as a platform for evaluating drug efficacy. C
ompared to clinical-used irinotecan (whose active ingredient is also SN3
8), after intravenous injection, Compound 10 only requires 20% of SN38 t
o kill 80% of in situ colorectal cancer and inhibit cancer cell growth, demo
nstrating significant and superior anti-tumor activity. Pharmacokinetic an
d distribution studies also show that Compound 10 can accumulate precis
ely in colorectal cancer tissue, releasing a higher concentration of SN38 in
the tumor than irinotecan. This result has a positive correlation with anima
l efficacy, represented by Compound 10's ability to target the tumor and
selectively enter the cancer cells to exert its toxic effect. Safety assessment
of Compound 10 in mice after treatment showed no abnormalities in the
heart, liver, spleen, lungs, kidneys, stomach, or small intestine. Based on th
e above results, our Compound 10 can specifically target colorectal cancer
and is safe.