The first line of treatment for advanced prostate cancer is androgen removal, but the disease progresses to destructive prostate cancer after 18 to 20 months with a median survival of only 1 to 2 years. Prior to 2004, the field of CRPC treatment was slow to develop, with chemotherapy and radiotherapy being used for CRPC. Since 2004, the field of CRPC treatment has developed rapidly, and some new treatment methods and tools have gradually entered clinical validation or use, and some drugs have been approved by the FDA and marketed abroad, which has greatly increased the choice of CRPC treatment and also brought new challenges. This paper introduces and compares these drugs so that we can better understand them and make a better choice in the future treatment process with patients’ own conditions. The main drug currently used in the treatment of prostate cancer is docetaxel, which mainly acts on the microtubules of tumor cells and causes apoptosis by blocking cell mitosis. A multicenter study of patients with CRPC has shown some efficacy. However, due to genetic or acquired drug resistance, some patients are ineffective and some are effective on initial therapy but the disease will eventually progress. Nowadays, the newly launched cabazitaxel is a new generation of semi-synthetic paclitaxel, and preclinical studies have shown its activity against docetaxel-resistant tumor cells and tumor models. The TROPIC-based study also showed that cabazitaxel + prednisone prolonged the survival of CRPC patients with disease progression during and after docetaxel-based regimens, and the FDA approved cabazitaxel for use in CRPC patients with disease progression after docetaxel treatment. Although the cabazitaxel plus prednisone regimen has good efficacy, this regimen is also associated with more serious toxicities. The more serious toxic side effects of this drug are mainly neutropenia, so the application of this drug requires careful consideration of the risk-effect ratio by clinicians. In the past, CRPC was considered to be androgen-independent, but there is evidence that androgen concentrations in prostate cancer tissues are maintained at low levels, sufficient to activate androgen receptor (AR)-mediated signal transduction pathways and expression of related genes, even when serum testosterone reaches depleted levels. Because most tumors at this stage still rely on the AR signaling pathway for growth, it is inappropriate to call this stage androgen non-dependent prostate cancer. Previously, the residual androgens in prostate tissue after androgen depot treatment were thought to be derived from the uptake and conversion of adrenal androgens, and ketoconazole was preferred to inhibit the action of cytochrome P45014α demethylase to effectively control adrenal-derived testosterone production. However, recent studies in recent years have shown that metastatic foci of CRPC are able to use cholesterol or steroid precursors for their own androgen biosynthesis. CYP-17A is a key enzyme in the androgen synthesis pathway that converts pregnenolone and progesterone to the weak androgenic hormones dehydroepiandrosterone and androstenedione, and plays an important catalytic role in both possible pathways. Abiraterone, a pregnenolone derivative, is a selective, high-affinity, irreversible inhibitor of CYP-17A. Abiraterone acetate is able to improve oral bioavailability. A multicenter phase II study of abiraterone acetate in combination with prednisone in patients with CRPC after docetaxel treatment has also shown significant efficacy. In the recently reported phase III clinical trial, 1195 patients with CRPC who failed docetaxel treatment were observed. Subjects received abiraterone acetate (1000 mg once daily) + prednisone (5 mg twice daily), and abiraterone prolonged overall survival by 4 months compared with the placebo group, and abiraterone was well tolerated. The most common toxicities were hypertension, hyperkalemia and The most common side effects were hypertension, hyperkalemia and fluid retention, which were significantly reduced with the addition of low-dose prednisone. Abiraterone has been approved by the FDA for the treatment of patients with CRPC who have failed docetaxel therapy with metastasis. TAK-700, another CYP-17A inhibitor, has been shown in animal studies to have a greater ability to inhibit androgen production and to be more selective. Theoretically, TAK-700 has a higher clinical value than abiraterone, but clinical trials are needed to verify its efficacy. MDV-3100 is a new AR blocker that blocks the AR signaling pathway by blocking androgen and receptor binding, inhibiting AR nuclear translocation and inhibiting the recruitment of co-stimulatory factors. It has shown good efficacy and tolerability in phase I and II clinical studies, regardless of whether CRPC patients have received prior chemotherapy. MDV-3100 is a pure androgen antagonist and, unlike bicalutamide, has no agonistic activity. MDV-3100 also has the advantage that it can be used without the need for steroids, which is not the case with abiraterone acetate (because steroids reduce the risk of infection and osteoporosis associated with long-term use of abiraterone acetate). Therefore, the indication for MDV-3100 may be in metastatic CRPC. New Advances in Immunotherapeutic Drugs Sipuleucel-T is an autologous vaccine prepared by isolating dendritic cells from peripheral blood of patients. The results of clinical trials showed that Sipuleucel-T treatment significantly improved the median survival of prostate cancer patients to 25.9 months compared to 21.4 months in the control group, but did not significantly improve the survival of patients. Therefore, the FDA approved Sipuleucel-T for the treatment of asymptomatic or mildly symptomatic patients with metastatic CRPC and metastatic hormone-resistant prostate cancer. New Advances in Bone Targeted Drug Therapy Prostate cancer is one of the solid tumors most prone to bone metastasis, and more than 90% of patients with metastatic CRPC have bone metastasis. The symptoms of bone metastases and the bone-related events caused by them can reduce the quality of life of patients, lead to the impairment of normal functions, and even accelerate death. Therefore, bone microenvironment is an important target for CRPC treatment. Currently, zoledronic acid is the main drug used to relieve bone destruction in prostate cancer patients with bone metastases in China, but a randomized-double-blind clinical study confirmed that denosumab delayed bone-related events in tumor patients better than zoledronic acid. The median delay in bone-related events in prostate cancer patients was 21 months, compared with 17 months for zoledronic acid. The FDA approved Denosemide on November 19, 2010 for the treatment of bone metastases in advanced prostate cancer. ALSYMPCA is a randomized, double-blind, multinational, multicenter study of 809 patients randomized in a 2:1 ratio to alpharadin+best supportive care and placebo+best supportive care in patients with metastatic CRPC. The primary endpoint was overall survival, and secondary endpoints included time to first bone-related event, time to PSA progression, patient quality of life, and safety. 2011 European Society of Medical Oncology-European Cancer Organization (ESMO-ECCO) meeting reported the interim staging results of the ALSYMPCA study, with a median survival of 14.0 months in the treatment group and 11.2 months in the control group. Treatment with alpharadin reduced the risk of death by 3 (HR=0.7, P=0.00185), and patients tolerated alpharadin well with a low incidence of myelosuppression. Therefore, alpharadin has the potential to become one of the standard treatment options for patients with CRPC with bone metastases. Going forward, Sipuleucel-T may be preferred in CRPC with mild or no symptoms, provided that the patient is in good health. MDV-3100 also has many advantages as an endocrine therapy if the patient’s disease has progressed. Denosumab and alpharadin are both drugs we can consider in the case of bone metastases. If endocrine therapy is not effective, we can consider docetaxel and cabazitaxel, and if the disease progresses further, abiraterone can be an effective follow-up. At this time, the possibility of abiraterone being approved for use prior to docetaxel treatment needs to be explored, as most patients would like to delay chemotherapy, but there are many pressing issues that need to be addressed when abiraterone is given prior to chemotherapy. In addition to the above-mentioned drugs that have been approved by FDA or have completed phase III clinical studies, there are still many drugs in phase II and phase III clinical studies, and some of them will gradually enter the clinical application in the future, which will increase the choice of therapeutic drugs for CRPC patients and bring new challenges to clinicians. We should think about how to combine old and new drugs, the order of drug use, how to choose the best drug for each individual, and how to balance efficacy and adverse effects.