FARMASINO PHARMACEUTICALS (ANHUI) CO.,LTD Company Blog & News

As the Spring Festival of the Year of the Snake in 2025 approaches, I wish all our great partners a happy New Year! All the best!     

Pharmacology and Synthesis of Ruxolitinib   Pharmacology Ruxolitinib is a potent inhibitor of Janus-associated kinases (JAK) 1 and 2, which play crucial roles in the signaling pathways for various cytokines and growth factors involved in hematopoiesis and immune function. The dysregulation of JAK-STAT signaling is implicated in a range of hematologic malignancies and inflammatory disorders. Ruxolitinib exerts its therapeutic effects by selectively inhibiting the JAK1/2 enzymes, thereby reducing the phosphorylation and activation of STAT proteins. This inhibition ultimately leads to decreased transcription of pro-inflammatory and proliferative genes. Clinically, ruxolitinib is primarily used in the treatment of myeloproliferative disorders such as myelofibrosis and polycythemia vera. By targeting the aberrant JAK-STAT signaling pathway, ruxolitinib helps to alleviate symptoms such as splenomegaly, cytopenias, and constitutional symptoms, as well as to control hematocrit levels in patients. The drug is administered orally and is known for its rapid onset of action and manageable side effect profile, which includes cytopenias, infections, and elevation of liver enzymes.     Synthesis The synthesis of ruxolitinib involves multiple key steps, typically starting from commercially available starting materials. One of the common synthetic routes begins with the condensation of 4-(4-methylpiperazin-1-yl)-7H-pyrrolo[2,3-d]pyrimidine with a suitable aryl halide under Buchwald-Hartwig amination conditions. This reaction leads to the formation of an N-arylated pyrrolopyrimidine intermediate. The next crucial step involves the introduction of a cyano group at the appropriate position on the aryl ring, typically achieved through a nucleophilic substitution reaction using a suitable nitrile source. This is followed by the reduction of the cyano group to form the corresponding primary amine. Subsequent cyclization with a carboxylic acid derivative leads to the formation of a lactam ring, a key structural component of ruxolitinib. Final steps often include the purification of the desired product through crystallization or chromatography. The overall yield and purity of ruxolitinib can vary depending on the choice of reagents and conditions, but the outlined synthetic route is generally efficient and scalable.   Conclusion Ruxolitinib's pharmacological activity as a JAK1/2 inhibitor makes it a valuable therapeutic agent for managing specific myeloproliferative disorders. Its synthesis, while complex, is well-established and involves a series of strategic reactions to assemble the drug's unique molecular architecture. The continued study and development of JAK inhibitors like ruxolitinib hold promise for treating a variety of hematologic and inflammatory conditions.

CPHI & PMEC China is Asia’s leading pharmaceutical show for trading, knowledge sharing and networking. It spans all industry sectors along the pharmaceutical supply chain and is your one-stop platform to grow business in the 2nd largest pharma market in the world. CPHI & PMEC China 2024, with the co-located shows FDF, bioLIVE, Pharma Excipients, NEX and LABWORLD China, etc. is expected to draw 3,500+ exhibitors and hundreds and thousands of professionals from the pharmaceutical industry.   FarmaSino will participate in CPHI China 2024 and set up an exhibition at the exhibition at Booth E2A02. Farmasino Pharmaceuticals（Anhui）Co.,LTD is a wholly-owned subsidiary of Farmasino Co., Ltd. It is a high technology enterprise which specializes in the R&D, manufacturing and exporting of API and Advanced Intermediates.It was founded in October 2008 in Maanshan city, Anhui Province. In order to further expand production, it relocated to Suzhou Economic Development Zone, Anhui Province in August,2021. Now it occupies an area of 300 acres (200000m2). The total investment of the project is 1 billion RMB. It has established standardized chemical synthesis workshop which is in accordance with GMP requirements.   FarmaSino has its own R&D centers and pilot-scale workshop. According to the ISO9001:2008 Quality system by SGS, we carry out scientific management to provides one-stop services of research - development - production for a variety of fine chemicals and special chemicals. Not only do we make effective use of our strong technological strength, but also establish cooperative relations with several well-known companys and research institutions.   Welcome to our booth, we look forward to your visit. We will serve you wholeheartedly!

Apixaban is a novel oral anticoagulant. It is possible to directly, reversibly, and highly selectively block the active site of factor Xa, blocking the conversion of prothrombin to thrombin, and thereby preventing thrombosis. As compared with rivaroxaban, apixaban also prevents thrombosis by indirectly inhibiting thrombin-induced platelet aggregation and reducing thrombin production. It is mainly used to prevent venous thromboembolism events in adult patients undergoing elective hip or knee replacement. In addition to the indications listed above, it is used to reduce the risk of stroke and systemic embolism in patients with nonvalvular atrial fibrillation; To reduce the risk of deep vein thrombosis and recurrent pulmonary embolism; It is used to treat deep vein thrombosis and pulmonary embolism.   Absorption of apixaban is predominantly in the small intestine. There is a first-pass effect, and at an oral dose of 10mg, the absolute bioavailability of apixaban is approximately 50%, with no effect of food on its bioavailability. The plasma protein binding rate of apixaban in humans is about 87%, and it is mainly bound to albumin. The volume of distribution was about 21L and was mainly distributed in the extracellular fluid. The total plasma clearance was approximately 3.3L/h, and the renal clearance was approximately 0.9L/h, with an apparent elimination half-life of approximately 12h.   FarmaSino is a leader API and intermediates manufacturer in China. We can provide Apixaban API and intermediates with high quality and competitive price. Please visit our product list from more information.

On 6 Aprile 2024, Novo Nordisk published the result of STEP HFpEF DM on the New England Journal of Medicine. The results demonstrated that among patients with obesity-related heart failure with preserved ejection fraction and type 2 diabetes, semaglutide led to larger reductions in heart failure–related symptoms and physical limitations and greater weight loss than placebo at 1 year.

  API China focuses on improving the overall level of production, research and development of pharmaceutical raw materials, intermediates and pharmaceutical excipient in China, representing new products and technologies in China's pharmaceutical industry. API China has become a brand event that brings together industry leaders, exhibits advanced product technologies, interprets policies and regulations for enterprises, improves industry production levels and reflects industry development trends. The exhibition is supported by more than 97% of China's top 100 pharmaceutical industry enterprises, providing pharmaceutical enterprises with decision-making, procurement, technology, research and development personnel to establish information exchange and business cooperation opportunities with target customers.   From May 15 to 17, 2024, FarmaSino will sincerely welcome you at Booth 1.2Y96, the National Exhibition and Convention Center (Shanghai). We will bring our latest products, the most professional service, the most competitive price, the most warm reception and the most sincere friendship to visitors from all over the world. We sincerely welcome your visit and look forward to further cooperation and development with you. We wish people all over the world the same : ‘Better health, better life.’   Contents: Pharmaceutical raw materials, pharmaceutical accessories, natural extracts, chemical reagents, intermediates, fine chemical raw materials, important raw materials, food raw materials and additives, veterinary raw materials, feed raw materials and additives, health care raw materials and additives, biotechnology, pharmaceutical research and development services, contract customized production services, registration and pharmaceutical services, training services

As an important class of hypoglycemic and weight loss drugs, GLP-1 drugs have attracted much attention and made significant development in recent years. Since GLP-1 drugs were found to have hypoglycemic effects, GLP-1 targets have been firmly in the hot track, especially after the approval of semaglutide for weight loss indications, the research and development of GLP-1 drugs has reached the peak. In 2023, the market value of Novo Nordisk and Eli Lilly skyrocketed, and the core factor driving the market value skyrocketed was the popular GLP-1 drugs. With the increasing number of diabetes and obesity patients worldwide, the demand for GLP-1 drugs has great potential, and the research and development momentum at home and abroad is strong. In the future, GLP-1 drugs are expected to play a therapeutic role in fields such as cardiovascular disease and fatty liver.   In 1985, a peptide chain composed of 31 amino acids, natural GLP-1 was first discovered, but its half-life is very short, about 2 minutes, and it is easy to be degraded by DPP-4 enzyme after secretion into the blood. The development of GLP-1 receptor agonists needs to solve the problem of short half-life.   The first short-acting GLP-1RA, exenatide (Astrazeneca), was approved by the FDA in 2005. It has a half-life of about 3 hours and requires twice daily subcutaneous injections. In 2009, the first long-acting GLP-1 RA, liraglutide (Novo Nordisk), was launched as a once-daily subcutaneous injection. Once-weekly injections of dulaglutide (Eli Lilly) and semaglutide (Novo Nordisk) were approved in 2014 and 2017, respectively. In 2022, the dual-target GLP-1/GIP telpotide (Eli Lilly) was approved for marketing, which kicked off the prologue of dual targets.   GIP-1 receptors are widely distributed, and multiple mechanisms of GLP-1RA act together. Glucagon like peptide-1 (GLP-1) : A hormone secreted by intestinal L-cells that promotes insulin secretion by pancreatic β cells in a glucose concentration-dependent manner, and its receptor (GLP-1R) is widely distributed in many organs and tissues such as the central nervous system, cardiovascular system, muscle, and gastrointestinal tract.   The receptor agonist of GLP-1 (GLP-1RA) stabilizes blood glucose and reduces body weight through various glucose-lowering mechanisms. If it acts on the stomach, it can delay gastric emptying by inhibiting gastrointestinal peristalsis; It acts on the central nervous system (especially the hypothalamus) to increase satiety and inhibit appetite; It acts on the liver and inhibits hepatic glucose output. Promoting insulin to stimulate glucose uptake in peripheral tissues (increasing insulin sensitivity).

Top 30 Anti-tumor Drugs in 2023 (In billion dollars)   No. Drug name Company Main indications Sales Growth rate 1 Keytruda (pembrolizumab) MSD Melanoma, NSCLC, Bladder cancer, HNC 25.01 19.5% 2 Opdivo (nivolumab) BMS/ONO Melanoma, NSCLC, HNC 10.04 9.0% 3 Darzalex (daratumumab) Johnson & Johnson Multiple myeloma, AL amyloidosis 9.74 22.2% 4 Imbruvica (ibrutinib) Abbvie/Joshnson CLL/SLL, MCL, GVHD 6.86 -17.9% 5 Revlimid (lenalidomide) BMS MM, MDS, MCL, FL 6.10 -39.0% 6 Tagrisso (osimertinib) Astrazeneca T790M NSCLC 5.80 7.0% 7 Xtandi (enzalutamide) Astellas Prostate cancer 5.07 4.3% 8 Ibrance (palbociclib) Pfizer Breast cancer 4.75 -6.0% 9 Jakafi (ruxolitinib) Incyte/Norvatis Myelofibrosis, PV 4.31 8.7% 10 Imfinzi (durvalumab) Astrazeneca Urothelial carcinoma,NSCLC, SCLC etc 4.24 52.0% 11 Perjeta (Pertuzumab) Roche HER2+ breast cancer 4.21 1.0% 12 Tecentriq (atezolizumab) Roche Urothelial carcinoma,NSCLC, TNBC 4.21 9.0% 13 Verzenio (abemaciclib） Eli Lilly Breast cancer 3.86 56.0% 14 Pomalyst (pomalidomide) BMS Multiple myeloma 3.44 -2.0% 15 Lynparza (olaparib) Astrazeneca/MSD Ovarian cancer, Breast cancer, Pancreatic cancer, Prostate cancer 2.81 7.0% 16 Enhertu (trastuzumab deruxtecan) Daiichi Sankyo/AZ HER2+ breast cancer, HER2-low brease cancer 2.57 104.8% 17 Calquence (acalabrutinib) Astrazeneca Mantle cell lymphoma, CLL/SLL 2.51 22.0% 18 Erleada (apalutamide) Johnson & Johnson Prostate cancer 2.39 26.9% 19 Venclexta (venetoclax) Abbvie CLL, AML 2.29 13.9% 20 Revolade/Promacta (eltrombopag) Norvatis Thrombocytopenia 2.27 10.0% 21 Yervoy (ipilimumab) BMS Melanoma, RCC, CRC 2.24 5.0% 22 Kadcyla (trastuzumab Emtansine) Roche HER2+ breast cancer 2.19 4.0% 23 Xgeva (denosumab) Amgen Solid tumor bone metastasis 2.11 5.0% 24 Kisqali (Ribociclib) Norvatis HR+ breast cancer 2.08 75.0% 25 Lenvima (lenvatinib) Eisai/MSD DTC, HCC, Endometrial carcinoma 2.01 8.4% 26 Sprycel (dasatinib) BMS ALL, CML 1.93 -11.0% 27 Tafinlar+Mekinist (dabrafenib+trametinib） Norvatis Melanoma, NSCLC, ATC 1.92 11.0% 28 Tasigna (nilotinib) Norvatis CML 1.85 -3.0% 29 Herceptin (trastuzumab) Roche HER2+ breast cancer 1.82 -16.0% 30 Avastin (bevacizumab) Roche CRC, Breast cancer, Lung cancer, Ovarian cancer etc 1.76 -19.0%    

On 8 March, the U.S. Food and Drug Administration approved a new indication for use for Wegovy (semaglutide) injection to reduce the risk of cardiovascular death, heart attack and stroke in adults with cardiovascular disease and either obesity or overweight.     The FDA decision is based on the results of the landmark SELECT phase III cardiovascular outcomes trial that examined the effect of adding Wegovy® 2.4 mg or placebo to cardiovascular standard of care in adults with overweight and obesity with established CVD and without diabetes. Wegovy® 2.4 mg significantly reduced the risk for first occurrence of a three-part composite MACE endpoint consisting of cardiovascular death, non-fatal heart attack, or non-fatal stroke. The primary composite outcome occurred in 6.5% of patients treated with Wegovy® and 8.0% with placebo. The estimated relative risk reduction of MACE was 20% vs placebo (HR 0.80 [95% CI: 0.72, 0.90] p

Salcaprozate sodium (SNAC) is the sodium salt form of salcaprozate. It is used in the treatment of gastrointestinal disorders, especially gastrointestinal disorders caused by the malabsorption of dicarbonate-phosphate compounds. SNAC can also promote the absorption of drugs in gastrointestinal epithelial cells, and effectively cope with the obstacles to the absorption of oral peptide drugs, for instance Semaglutide.   Absorption of oral dose peptides by intestine is challenging due to the physiological effects of the gastrointestinal tract. Ingested peptides or proteins are broken down into amino acids by ph-sensitive proteases, which are then transported to the mucosa by the translocater. Large molecules of carbohydrates or lipids are decomposed into small molecules to promote intestinal absorption. The intestinal epithelium has the function of recognizing and absorbing bacteria, viruses and other pathogens. So complex cellular and mucus barriers are formed to limit the entry of foreign or harmful substances. Therefore, unfortunately, exogenous peptides or protein drugs are restricted to penetrate the intestinal epithelium and enter the circulation. In this case, SNAC and its related compounds are used as Permeation enhancers to deal with this problem. The mechanism that SNAC promotes the absorption of Active pharmaceutical ingredient (API) is still not fully understood. It is generally believed that SNAC improves the membrane permeability of gastrointestinal epithelial cells may be related to membrane perturbation, membrane fluidization, and changes in API solubility. It also may improve transcellular permeability by increasing its hydrophobic role through non-covalent bond binding to API.   The successful preparation of semaglutide tablets depends on its co-formulation with SNAC. SNAC promotes the monosomy of semaglutide, making it more permeable. For semaglutide molecules, most semaglutide exists in the form of oligomers in the stomach; However, SNAC triggered a change in polarity of the solution containing the dissolved tablet, weakening the hydrophobic interaction necessary for oligomerization. Since SNAC is lipophilic, it efficiently inserts into the cell membrane of the gastric epithelium, altering the intrinsic integrity of cholesterol phospholipids and proteins, which in turn affect the fluidity of the cell membrane. It was confirmed that SNAC enhances the intracellular uptake of semaglutide by gastric epithelial cells, thus supporting the notion that SNAC promotes transcellular transport of semaglutide. SNAC can effectively increase the local pH value around the semaglutide molecule in the stomach, prevent the degradation of peptides by pepsin, and make semaglutide penetrate the gastric mucosa and be absorbed into blood by the concentration gradient on the surface of the cell membrane. The use of SNAC is of great significance for oral semaglutide tablets. FarmaSino can provide high purity and high quality SNAC together with Semaglutide API* and intermediates include semaglutide-related fragments, main chains, and side chains of different steps. Please check following links for more information.

Semaglutide is an anti-diabetic drug which is used to treat type 2 diabetes and manage chronic weight. Semaglutide is a glucagon-like peptide-1(GLP-1) receptor agonist with 94% sequence homology with human GLP-1. It increases the production of insulin, which can lower the blood glucose level. Semaglutide also appears to enhance growth of β cells, sites of insulin production, in the pancreas. By lowering appetite and slowing down digestion in the stomach, Semaglutide also can reduce food intake to control body weight.   Semaglutide for injectable grade 99% is prepared for the formulation of Semaglutide injection. The purity of this product can reach 99.0% and the assay should reach 95%~105% with peptide content of Semaglutide 76%~100%. Semaglutide for oral grade 98% is suitable for the markets with high requirements of oral dose for the control of raw material impurities. The purity of this product should reach 98% with the same acceptance criteria of other standards with Semaglutide injectable grade 99%. Semaglutide for oral grade 96% is much more suitable for a price sensitive market where the tabbing process does not produce new impurities with its purity of 96%. The assay of this product should reach 90%~100%. Semaglutide crude product is prepared for the enterprises that have the production capacity and want to own the API approval. Semaglutide API can be obtained after purification by chromatography and freeze drying from Semaglutide crude product. The purity of this product should reach 50% and the assay over 35%.   Semaglutide secondary acylation intermediate is N-1 intermediate of Semaglutide. The protection group of this prodcut was deprotected to obtain Semaglutide crude product, which was purified by chromatography and freeze dried to obtain API. Secondary acylation intermediate is suitable for the enterprises that have the production capacity and want to own the API approval.   Semaglutide primary acylation intermediate and Semaglutide dipeptide are Semaglutide N-2 main chain intermediate and N-2 fragment. The primary acylation intermediate was acylated with Semaglutide dipeptide to obtain Semaglutide secondary acylation intermediate and further hydrolyzed to obtain Semaglutide crude product. Acylation, hydrolysis tank, high pressure chromatography system, drying equipment are required.   Semaglutide main chain P29 and Semaglutide side chain (tetrapeptide) are Semaglutide N-3 main chain intermediate and N-3 fragment. TheSemaglutide main chain P29 was acylated with Semaglutide side chain to obtain Semaglutide primary acylation intermediate. Further reaction was underwent to obtain the final API. These products are suitable for for the enterprises that have the production capacity and want to own the API approval. Acylation, hydrolysis tank, high pressure chromatography system, drying equipment are required. FarmaSino provides these the API with different grade and related intermediates of Semaglutide with reliable quality and competitive price.   Please get more information from following links: 910463-68-2: Semaglutide Semaglutide Starts the New Life with Type 2 Diabetes   *All APIs and intermediates for R&D use ONLY.

Farmasino adheres to the localization development of Algeria. It provides a one-stop solution for the local biopharmaceutical industry, from raw materials to registration documents, from production processes to pharmaceutical machinery. In 2023, its cumulative exports exceeded 20 million US dollars. Welcome to our booth for mutual benefit.