ORM-15341 CAS 1297537-33-7

What is ORM-15341?

Ketodarolutamide (ORM-15341) has garnered significant attention in the treatment of prostate cancer. It is a potent and highly affinity nonsteroidal androgen receptor competitive complete antagonist. Essentially, it is the major active metabolite of the next-generation anti-androgen product ODM-201 in the human body. In other words, after patients use ODM-201, the active compound is partially converted to ORM-15341, which also exhibits a very strong inhibitory effect on cancer activity.

Ketodarolutamide inhibits testosterone-induced AR nuclear translocation. Its excellent specificity interferes with the proliferation of AR-dependent prostate cancer cells and demonstrates antitumor activity in castration-resistant prostate cancer models.

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What is the mechanism of action of ORM-15341?

ORM-15341 is a nonsteroidal androgen receptor regulatory molecule and the main active metabolite produced after the oral compound ODM-201 enters the human body. After oral ingestion of ODM-201, it is metabolized in the body into Ketodarolutamide, which is the core active substance for its androgen receptor regulatory function.

It primarily acts on the androgen receptor, a key target for the proliferation of prostate cancer cells. Related experimental data confirm that ORM-15341(Ketodarolutamide) has a strong affinity for the androgen receptor, with a half-maximal inhibitory concentration (IC50) of 38 nanomoles per liter and a competitive binding constant of 8 nanomoles per liter, demonstrating superior efficacy compared to enzalutamide and apalutamide.

Even against androgen receptor mutants with weakened efficacy in many commonly used products, ORM-15341 can still exert its regulatory effect normally, laying the experimental foundation for its application in castration-resistant prostate cancer. Simultaneously, it can inhibit androgen-induced androgen receptor nuclear translocation, maintaining stable autoregulatory activity even in prostate cancer cells with androgen receptor overexpression.

Due to the low blood-brain barrier penetration of its parent compound ODM-201, Ketodarolutamide produces almost no significant central nervous system-related effects in vivo and does not significantly disrupt the human androgen feedback loop. Clinical studies have shown that in metastatic castration-resistant prostate cancer patients treated with ODM-201 who had not received other treatments, 86% of patients experienced a 50% or greater reduction in prostate-specific antigen (PSA) levels compared to their initial values. This positive effect is closely related to the androgen receptor regulatory activity inherent in ORM-15341 itself.

Will ORM-15341 affect normal androgen levels in the body?

According to existing research, ORM-15341 does not affect normal androgen levels in the body.

In animal studies targeting its parent compound, ODM-201, it was found that this compound does not interfere with the androgen feedback loop of the hypothalamus-pituitary-gonadal axis. In other words, ODM-201 and its metabolite ORM-15341(Ketodarolutamide), while interfering with androgen receptor signaling, do not affect the body's normal hormone regulatory centers, and therefore do not cause abnormal fluctuations in serum testosterone levels.

It is an androgen receptor antagonist. Its mechanism of action is to directly bind to androgen receptors, blocking the opportunity for androgens to bind to the receptors, rather than affecting androgen synthesis or secretion. Simply put, it does not reduce the amount of androgens, but rather occupies the androgen receptors, preventing androgens from binding.

This mode of action makes ORM-15341 significantly different from some earlier anti-androgen products, and the former is more effective.

Furthermore, the parent compound of ORM-15341, ODM-201, has a very low blood-brain barrier penetration rate, which further reduces its potential impact on the central nervous system and endocrine regulatory centers.

In summary, ORM-15341(Ketodarolutamide)'s action is precisely limited to the receptor level, exerting its effects without disrupting overall endocrine balance and helping to maintain normal hormonal homeostasis in patients.

MF of ORM-15341

Melting point	210 - 212C
Boiling point	714.7±60.0 °C(Predicted)
Density	1.41±0.1 g/cm3(Predicted)
Molecular weight	396.83
Storage conditions	-20°C Freezer, Under inert atmosphere
Acidity coefficient	8.70±0.10

Specification

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FAQ:

Q1: How effective is ORM-15341 in inhibiting androgen receptors?
In vitro experimental data show that Ketodarolutamide achieves a half-maximal inhibitory concentration (IC50) of approximately 38 nanomoles on the androgen receptor, corresponding to a binding inhibition constant of only 8 nanomoles. Under the same experimental conditions, the corresponding value for similar second-generation active ingredients is 86 nanomoles, demonstrating that its binding efficacy to the receptor is more than ten times higher. Furthermore, it maintains a stable and highly effective effect against various receptor variants, making it suitable for most use cases where tolerance may develop.
Q2: What are the advantages of ORM-15341?
Studies have shown that the brain-to-plasma concentration ratio of ORM-15341(Ketodarolutamide) is extremely low, thus it almost never enters the central nervous system. Therefore, it has extremely low blood-brain barrier penetration, which is its greatest advantage.
Q3: Is ORM-15341 effective when used alone?

ORM-15341 can be used alone on a daily basis to exert its effects directly. It can act stably on the corresponding receptors, accurately block related signal transduction, and smoothly regulate the body's related physiological states.

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