fruqintinib

Fruquintinib (Fruzaqla, Takeda Pharmaceuticals, Inc.) was approved by the US Food and Drug Administration (FDA) on 8 November 2023.

Clinical data:
– Drug class: Antineoplastic
– ATC code: L01EK04 (WHO)

Legal status:
– US: ?-only

This information is intended for adult patients with metastatic colorectal cancer (mCRC) who have previously undergone chemotherapy with fluoropyrimidine, oxaliplatin, and irinotecan, as well as received anti-VEGF therapy. Additionally, if the patient is RAS wild-type and it is medically suitable, they may have also received anti-EGFR therapy. Please refer to the complete prescribing information for fruquintinib.

Colchicine, also known as Colcrys or Mitigare, is a medication prescribed for the treatment and prevention of gout, a form of arthritis that causes severe pain. Nitroglycerin, morphine, phenazopyridine, phenobarbital, potassium chloride, and sodium fluoride are other medications that may be used for various medical purposes.

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The FDA granted approval to trilaciclib (Cosela, G1 Therapeutics) on February 12th, 2021. This drug is a cyclin-dependent kinase 4/6 inhibitor (CDK4/6) and is intended to reduce the occurrence of chemotherapy-induced myelosuppression (CIM) in adult patients diagnosed with extensive-stage small-cell lung cancer (ES-SCLC). Trilaciclib is specifically recommended for patients who are undergoing treatment with platinum/etoposide-containing or topotecan regimens.

The selection of adjuvant treatments for mCRC patients depends on factors such as tumor stage, high-risk pathologic characteristics, microsatellite instability status, patient age, and performance status. The primary systemic treatments for mCRC include chemotherapy, targeted therapy, and immunotherapy.

Objective: This drug review aims to evaluate the effectiveness and safety of opicapone, a newly FDA approved catechol-O-methyl transferase (COMT) inhibitor, for the treatment of end-of-motor motor fluctuation in adults with Parkinson’s disease.

Bosutinib (Bosulif, Pfizer) has been approved by the Food and Drug Administration on September 26, 2023. This approval is specifically for pediatric patients who are 1 year of age and older and have chronic phase (CP) Ph+ chronic myelogenous leukemia (CML). The drug is indicated for patients who are newly diagnosed (ND) or have shown resistance or intolerance (R/I) to prior therapy.

There are two groups of drugs. The first group consists of seven FDA-approved EGFR-TKIs, namely afatinib, brigatinib, dacomitinib, neratinib, osimertinib, pyrotinib, and vandetanib. The second group includes four drugs approved for cancer treatment outside of the USA.

According to a press release from Teva Pharmaceuticals, the FDA has granted approval for a generic version of Forteo for specific patients with osteoporosis.

FDA Approval: Understanding its Significance

When a drug receives FDA approval, it signifies that the data regarding its effects has undergone a thorough review by the CDER (Center for Drug Evaluation and Research). This evaluation process ensures that the drug is deemed to offer benefits that surpass its known and potential risks for the specific population it is intended for.

The fruquintinib group had a median overall survival of 7.4 months (95% CI 6.7-8.2), while the placebo group had a median overall survival of 4.8 months (95% CI 4.0-5.8). The hazard ratio was 0.66 (95% CI 0.55-0.80; p<0.0001).

The main goal of the study was to measure overall survival [OS], and it successfully achieved this with a hazard ratio [HR] of 0.66. This led to a significant improvement in OS, increasing from approximately 4.8 months in the placebo group to about 7.4 months in the fruquintinib group.

Survival statistics are utilized by doctors to assess a patient’s prognosis, or chance of recovery. These statistics also aid in the evaluation of treatment options. Typically, researchers provide survival statistics as rates for specific types of cancer.

75% of people diagnosed with soft tissue sarcomas survive their cancer for 1 year or more, while almost 55% survive for 5 years or more.

Surgical resection is an effective treatment option for achieving long-term survival in patients with colorectal liver metastases (CRLM), as it has been shown to result in a 5-year survival rate ranging from 40% to 50%.

On the other hand, a majority of the individuals who were treated with ARPI therapy subsequently underwent Pluvicto treatment after their cancer advanced. This is likely the reason why patients in the control group had a nearly identical, and slightly better, median overall survival of 19.71 months.

The researchers noted that the median overall survival for the 2.5 mg/kg cohort was 15.3 months, for the 3.4 mg/kg cohort was 14.0 months, and for the lyophilized cohort was 24.5 months. They also mentioned that these outcomes are favorable compared to what is typically observed in heavily pretreated patients.

Results: Out of the 521 patients who were randomly assigned, the median overall survival was 34.9 months (95% CI, 28.8 to 40.0) in the group that received palbociclib-fulvestrant and 28.0 months (95% CI, 23.6 to 34.6) in the group that received placebo-fulvestrant. The hazard ratio for death was 0.81 (95% CI, 0.64 to 1.03; P=0.09).

Bevacizumab is designed to target the protein VEGF, which is found in cancer cells. VEGF plays a crucial role in promoting the growth of blood vessels that supply nutrients and oxygen to cancer cells, enabling their survival and proliferation.

Fruquintinib is a new type of small-molecule anti-VEGFR drug that specifically targets VEGFR-1, -2, and -3. Its main purpose is to inhibit the process of angiogenesis, which is crucial for supplying oxygen and nutrients to cancer cells. The VEGF/VEGFR pathway plays a vital role in this process.

Clinical data for Fruquintinib, also known as HMPL-013, includes information on its license data in the US. It is administered orally and belongs to the drug class of antineoplastics.

Fruquintinib, marketed as ELUNATE, is an oral inhibitor of VEGFR 1/2/3, which are crucial in blocking tumor angiogenesis. It was granted approval by the China National Medical Products Administration (NMPA) in September 2018.

Floxuridine is quickly metabolized to produce 5-fluorouracil, which is the active ingredient of the drug. The main mechanism of action of 5-fluorouracil is to disrupt DNA synthesis. Additionally, it may also hinder the production of faulty RNA by physically integrating into the RNA structure.

Fruquintinib, also known as HMPL-013 and with a CAS Number of 1194506-26-7, is available from Cayman Chemical.

Regorafenib is an oral multikinase inhibitor that targets angiogenesis, cell proliferation, and tumor stroma by inhibiting VEGFR1-3, TIE2, FGFR1, PDGFR?², c-KIT, RET, c-RAF/RAF-1, and BRAF V600E.

Sabizabulin disrupts the cytoskeleton by targeting the colchicine binding site on ? tubulin. It also binds strongly to a unique site on ? tubulin, causing cross-linking between ? and ? tubulin subunits of microtubules. This inhibits microtubule formation and leads to microtubule depolymerization (59, 11, 16).