Apalutamide (ARN-509, JNJ-56021927) CAS 956104-40-8 High Purity API Raw Material

Apalutamide More Info

Apalutamide is a next-generation, nonsteroidal antiandrogen drug primarily indicated for the treatment of prostate cancer . Marketed under the brand name Erleada®, it was the first agent approved by the U.S. Food and Drug Administration for the specific indication of non-metastatic castration-resistant prostate cancer (nmCRPC) . It is also approved for use in metastatic castration-sensitive prostate cancer (mCSPC) . Chemically, its molecular formula is C21H15F4N5O2S, and it has a molecular weight of approximately 477.44 g/mol . The compound is also known by its developmental codes ARN-509 and JNJ-56021927 .

The primary mechanism of action of apalutamide involves direct and potent inhibition of the androgen receptor (AR), which plays a critical role in the growth and progression of prostate cancer cells . It binds directly to the ligand-binding domain of the AR, a step that prevents receptor nuclear translocation, inhibits its subsequent binding to DNA, and ultimately impedes AR-mediated transcription of genes that promote tumor cell proliferation . This activity leads to decreased tumor cell growth and increased apoptosis (programmed cell death). Notably, apalutamide binds to the AR with a 7- to 10-fold greater affinity than the first-generation antiandrogen bicalutamide, and it lacks the agonist activity that can sometimes limit the efficacy of older agents .

Clinically, apalutamide has demonstrated significant efficacy in improving outcomes for patients with prostate cancer. In the pivotal phase 3 SPARTAN trial, the addition of apalutamide to androgen deprivation therapy (ADT) in patients with nmCRPC resulted in a substantial improvement in median metastasis-free survival (MFS), extending it from 16.2 months with placebo to 40.5 months . A subsequent study specifically in Chinese patients confirmed these benefits, showing that apalutamide reduced the risk of prostate-specific antigen (PSA) progression by 76.7% compared to placebo . The standard dosage is 240 mg (four 60 mg tablets) taken orally once daily, with or without food, and it is typically used in conjunction with a gonadotropin-releasing hormone (GnRH) analog or after bilateral orchiectomy .

The pharmacokinetic profile of apalutamide supports its once-daily dosing. It is rapidly absorbed, reaching peak plasma concentrations approximately 2 hours after oral administration, and its absolute bioavailability is 100% . The drug is highly protein-bound (96%) and has a long half-life of approximately 3 days at steady state, which is reached after about 4 weeks of daily dosing . Apalutamide is extensively metabolized in the liver, primarily by the cytochrome P450 enzymes CYP2C8 and CYP3A4, to an active major metabolite, N-desmethyl apalutamide, which exhibits about one-third the activity of the parent compound . Approximately 65% of a dose is excreted in urine, and 24% in feces .

The safety profile of apalutamide is well-characterized and requires proactive management. The most common adverse effects reported in clinical trials and practice include fatigue, musculoskeletal pain (arthralgia), hot flushes, diarrhea, and skin rash . More specific toxicities requiring monitoring include hypothyroidism, falls and fractures, and potential seizure risk due to weak antagonism of the GABAA receptor at therapeutic levels . In a real-world observational study, 94% of patients reported at least one adverse event, with hot flushes, asthenia, and arthralgia being the most frequent . Importantly, a resistance mutation in the androgen receptor (p.F877L) has been identified, which can convert apalutamide from an antagonist to an agonist, leading to acquired drug resistance in some patients .

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