
LOXO-305 CAS No.:2101700-15-4
Pirtobrutinib (LOXO-305, LY3527727, RXC-005) is a highly potent and selective non-covalent BTK inhibitor with IC50 of 5.69 nM, shows nanomolar potency against both wild-type and C481-mutated BTK
Description
LOXO-305 CAS No.: 2101700-15-4 - An Overview
LOXO-305 is a highly effective and innovative drug used in the treatment of various types of cancer, including solid tumors. It is the latest generation of highly selective RET inhibitors with a low IC50 value.
As a manufacturer in China, we are proud to supply high-quality LOXO-305 to international markets. Our product has been tested and approved by the relevant authorities to meet the highest quality standards.
In this article, we will highlight the main features and benefits of LOXO-305 and explain why it is an excellent choice for cancer treatment.
LOXO-305 - Function
LOXO-305 inhibits various RET mutant forms, which are involved in the development of various types of cancer, including lung cancer, thyroid cancer, pancreatic cancer, breast cancer, and others. It works by binding to the active site of RET, thereby preventing cancer cells from proliferating and spreading to other parts of the body.
LOXO-305 - Efficacy
Studies have shown that LOXO-305 is highly effective in treating RET-driven tumors, with an objective response rate of 67% in patients with RET fusion-positive non-small cell lung cancer. It is also effective in treating other RET-altered cancers, including medullary thyroid cancer, papillary thyroid cancer, and others.
LOXO-305 - Safety
LOXO-305 has been demonstrated to be a safe and well-tolerated drug, with manageable side effects. The most common adverse events reported in clinical trials were hypertension, fatigue, diarrhea, and constipation.
LOXO-305 - Dosage and Administration
The recommended dosage of LOXO-305 for adult patients is 160 mg orally twice daily with or without food. It is available in capsule form and should be taken at the same time each day.
LOXO-305 - Clinical Trials
Clinical trials have shown promising results for LOXO-305 in the treatment of various types of cancer. The LIBRETTO-001 trial, for example, demonstrated that LOXO-305 had an objective response rate of 77% in patients with RET fusion-positive thyroid cancer.
LOXO-305 - Market Potential
There is significant potential for LOXO-305 in the global cancer drug market, given its high efficacy and safety profile. Lung cancer, for example, is the most common cancer worldwide, with around 2 million new cases diagnosed each year. As a highly effective drug for RET-driven lung cancer, LOXO-305 has the potential to make a significant impact on cancer treatment globally.
Conclusion
LOXO-305 is a highly effective and innovative drug used in the treatment of various types of cancer, including solid tumors. It works by inhibiting the development of cancer cells, preventing their proliferation and spread. With a high objective response rate and a manageable side effect profile, LOXO-305 has excellent potential in the global cancer drug market. As a manufacturer in China, we are proud to supply high-quality LOXO-305 to international markets, meeting the highest quality standards.

Pirtobrutinib (LOXO-305, LOXO305, LY3527727, RXC-005)
Catalog No.: URK-V963 Only Used For Lab.
Pirtobrutinib (LOXO-305, LY3527727, RXC-005) is a highly potent and selective non-covalent BTK inhibitor with IC50 of 5.69 nM, shows nanomolar potency against both wild-type and C481-mutated BTK
Biological Activity
Pirtobrutinib (LOXO-305, LY3527727, RXC-005) is a highly potent and selective non-covalent BTK inhibitor with IC50 of 5.69 nM.
LOXO-305 shows nanomolar potency against both wild-type and C481-mutated BTK.
LOXO-305 displays >300 fold selectivity on BTK over 98% of other kinases, reducing the potential for off-target toxicities.
Pirtobrutinib (LOXO-305) has been designed to maintain greater than 90% of maximal BTK inhibition at trough, thereby achieving effective target inhibition throughout the dosing interval, even in proliferative tumours.
Physicochemical Properties
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M.Wt |
479.436 |
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Formula |
C22H21F4N5O3 |
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CAS No. |
2101700-15-4 |
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Storage |
Solide Powder -20 °C 3years; 4°C 2years |
In Solvent -80°C 6 Months -20°C 1 Months |
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Solubility |
10 mM in DMSO |
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Chemical Name |
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References
1. Brandhuber B, et al. Clin. Lymphoma Myeloma Leuk. 2018;18:S216.
2. Ito K, et al. Eur J Cancer. 2021 Mar;145:183-193.
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