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Gemcitabine | CAS No: 95058-81-4 | GMP-certified suppliers
A medication that provides first-line or combination chemotherapy for advanced ovarian, metastatic breast, non-small cell lung, pancreatic, and bladder cancers.
Therapeutic categories
Primary indications
- Gemcitabine is a chemotherapeutic agent used as monotherapy or in combination with other anticancer agents
- In combination with [carboplatin], it is indicated for the treatment of advanced ovarian cancer that has relapsed at least 6 months after completion of platinum-based therapy
- Gemcitabine in combination with [paclitaxel] is indicated for the first-line treatment of patients with metastatic breast cancer after failure of prior anthracycline-containing adjuvant chemotherapy, unless anthracyclines were clinically contraindicated
Product Snapshot
- Gemcitabine is an injectable antineoplastic agent primarily available as a lyophilized powder or solution for intravenous administration
- It is indicated for the treatment of multiple advanced cancers including non-small cell lung cancer, pancreatic adenocarcinoma, ovarian cancer, metastatic breast cancer, and bladder transitional cell carcinoma, either as monotherapy or in combination with other chemotherapeutics
- Gemcitabine holds regulatory approval in key markets including the United States and Canada
Clinical Overview
Clinically, gemcitabine is employed as a chemotherapeutic agent for multiple malignancies. It is FDA-approved for use as monotherapy or in combination regimens. Indications include advanced ovarian cancer in combination with carboplatin following relapse six months after platinum-based therapy, metastatic breast cancer combined with paclitaxel post-anthracycline failure, non-small cell lung cancer (NSCLC) in combination with cisplatin, and pancreatic adenocarcinoma as first-line monotherapy. It is also utilized in combination with cisplatin for transitional cell carcinoma of the bladder. Investigational use in other tumor types is ongoing.
Pharmacodynamically, gemcitabine induces apoptosis primarily by inhibiting DNA synthesis at the G1/S phase transition. The triphosphate metabolite competes with deoxycytidine triphosphate for incorporation into DNA, causing masked chain termination. Additionally, gemcitabine diphosphate inhibits ribonucleotide reductase, decreasing endogenous deoxynucleotide pools and enhancing the incorporation of gemcitabine metabolites. This self-potentiating mechanism distinguishes it from other cytidine analogs such as cytarabine.
Absorption following intravenous administration leads to rapid systemic distribution. Gemcitabine is metabolized intracellularly; its metabolites accumulate to exert cytotoxic effects. Elimination primarily occurs via renal excretion of metabolites.
Safety considerations include dose-limiting myelosuppression, manifesting as anemia, neutropenia, leukopenia, and thrombocytopenia. Elevations in hepatic transaminases and alkaline phosphatase have also been documented. Myelosuppressive events rarely necessitate treatment discontinuation.
Gemcitabine is marketed chiefly as Gemzar in injectable formulations. Due to its narrow therapeutic index and potential for myelosuppression, strict adherence to dosing protocols and monitoring is essential.
For API procurement, it is critical to ensure high purity and compliance with pharmacopeial standards to mitigate variability impacting clinical safety and efficacy. Given gemcitabine’s sensitivity to degradation, API stability data and validated manufacturing processes should be reviewed diligently prior to sourcing.
Identification & chemistry
| Generic name | Gemcitabine |
|---|---|
| Molecule type | Small molecule |
| CAS | 95058-81-4 |
| UNII | B76N6SBZ8R |
| DrugBank ID | DB00441 |
Pharmacology
| Summary | Gemcitabine is a deoxycytidine analog that exerts antineoplastic effects by incorporating into DNA, causing masked chain termination and triggering apoptosis in proliferating malignant cells. It also inhibits ribonucleotide reductase, reducing deoxynucleotide pools to enhance incorporation of its active metabolites into DNA. This dual mechanism disrupts DNA synthesis and repair, resulting in cell cycle arrest at the G1/S transition and cytotoxicity across multiple tumor types. |
|---|---|
| Mechanism of action | Gemcitabine is a potent and specific deoxycytidine analog. After uptake into malignant cells, gemcitabine is phosphorylated by deoxycytidine kinase to form gemcitabine monophosphate, which is then converted to the active compounds, gemcitabine diphosphate (dFdCDP) and gemcitabine triphosphate (dFdCTP). These active metabolites are nucleosides that mediate antitumour effects. dFdCTP competes with deoxycytidine triphosphate (dCTP) for incorporation into DNA, thereby competitively inhibiting DNA chain elongation. The non-terminal position of dFdCTP in the DNA chain prevents detection of dFdCTP in the chain and repair by proof-reading 3′5′-exonuclease: this process is referred to as "masked DNA chain termination." Incorporation of dFdCTP into the DNA chain ultimately leads to chain termination, DNA fragmentation, and apoptotic cell death of malignant cells. Gemcitabine has self-potentiating pharmacological actions that can increase the probability of successful incorporation of gemcitabine triphosphate into the DNA chain: dFdCDP inhibits ribonucleotide reductase, an enzyme responsible for catalyzing the reactions that generate dCTP for DNA synthesis. Since dFdCDP reduces the levels of dCTP, there is less competition for gemcitabine triphosphate for incorporation into DNA. Gemcitabine can also reduce metabolism and elimination of active metabolites from the target ce1l, prolonging high intracellular concentrations of the active metabolites. Such self-potentiating effects are not present with [cytarabine]. |
| Pharmacodynamics | Gemcitabine is a nucleoside analog that mediates its antitumour effects by promoting apoptosis of malignant cells undergoing DNA synthesis. More specifically, it blocks the progression of cells through the G1/S-phase boundary. Gemcitabine demonstrated cytotoxic effects against a broad range of cancer cell lines _in vitro_. It displayed schedule-dependent antitumour activity in various animal models and xenografts from human non-small cell lung cancer (NSCLC) and pancreatic cancer. Therefore, the antineoplastic effects of gemcitabine are enhanced through prolonged infusion time rather than higher dosage. Gemcitabine inhibited the growth of human xenografts from carcinoma of the lung, pancreas, ovaries, head and neck, and breast. In mice, gemcitabine inhibited the growth of human tumour xenografts from the breast, colon, lung or pancreas by 69 to 99%. In clinical trials of advanced NSCLC, gemcitabine monotherapy produced objective response rates ranging from 18 to 26%, with a median duration of response ranging from 3.3 to 12.7 months. Overall median survival time was 6.2 to 12.3 months. The combined use of cisplatin and gemcitabine produced better objective response rates compared to monotherapy. In patients with advanced pancreatic cancer, objective response rates in patients ranged from 5.to 12%, with a median survival duration of 3.9 to 6.3 months. In Phase II trials involving patients with metastatic breast cancer, treatment with gemcitabine alone or with adjuvant chemotherapies resulted in response rate ranging from 13 to 42% and median survival duration ranging from 11.5 to 17.8 months. In metastatic bladder cancer, gemcitabine has a response rate 20 to 28%. In Phase II trials of advanced ovarian cancer, patients treated with gemcitabine had response rate of 57.1%, with progression free survival of 13.4 months and median survival of 24 months. Gemcitabine causes dose-limiting myelosuppression, such as anemia, leukopenia, neutropenia, and thrombocytopenia; however, events leading to discontinuation tend to occur less than 1% of the patients. Gemcitabine can elevate ALT, AST and alkaline phosphatase levels. |
Targets
| Target | Organism | Actions |
|---|---|---|
| DNA | Humans | cross-linking/alkylation |
| Ribonucleoside-diphosphate reductase large subunit | Humans | inhibitor |
| Thymidylate synthase | Humans | inhibitor |
ADME / PK
| Absorption | Peak plasma concentrations of gemcitabine range from 10 to 40 mg/L following a 30-minute intravenous infusion, and are reached at 15 to 30 minutes. One study showed that steady-state concentrations of gemcitabine showed a linear relationship to dose over the dose range 53 to 1000 mg/m<sup>2</sup>. Gemcitabine triphosphate, the active metabolite of gemcitabine, can accumulate in circulating peripheral blood mononuclear cells. In one study, the C<sub>max</sub> of gemcitabine triphosphate in peripheral blood mononuclear cells occurred within 30 minutes of the end of the infusion period and increased increased proportionally with gemcitabine doses of up to 350 mg/m<sup>2</sup>. |
|---|---|
| Half-life | Following intravenous infusions lasting less than 70 minutes, the terminal half-life ranged from 0.7 to 1.6 hours. Following infusions ranging from 70 to 285 minutes, the terminal half-life ranged from 4.1 to 10.6 hours. Females tend to have longer half-lives than male patients. Gemcitabine triphosphate, the active metabolite of gemcitabine, can accumulate in circulating peripheral blood mononuclear cells. The terminal half-life of gemcitabine triphosphate, the active metabolite, from mononuclear cells ranges from 1.7 to 19.4 hours. |
| Protein binding | Gemcitabine plasma protein binding is less than 10%. |
| Metabolism | Following administration and uptake into cancer cells, gemcitabine is initially phosphorylated by deoxycytidine kinase (dCK), and to a lower extent, the extra-mitochondrial thymidine kinase 2 to form gemcitabine monophosphate (dFdCMP). dFdCMP is subsequently phosphorylated by nucleoside kinases to form active metabolites, gemcitabine diphosphate (dFdCDP) and gemcitabine triphosphate (dFdCTP). Gemcitabine is also deaminated intracellularly and extracellularly by cytidine deaminase to its inactive metabolite 2′,2′-difluorodeoxyuridine or 2´-deoxy-2´,2´-difluorouridine (dFdU). Deamination occurs in the blood, liver, kidneys, and other tissues, and this metabolic pathway accounts for most of drug clearance. |
| Route of elimination | Gemcitabine mainly undergoes renal excretion. Within a week following administration of a single dose of 1000 mg/m<sup>2</sup> infused over 30 minutes, about 92-98% of the dose was recovered in urine where 89% of the recovered dose was excreted as difluorodeoxyuridine (dFdU) and less than 10% as gemcitabine. Monophosphate, diphosphate, or triphosphate metabolites of gemcitabine are not detectable in urine. In a single-dose study, about 1% of the administered dose was recovered in the feces. |
| Volume of distribution | In patients with various solid tumours, the volume of distribution increased with infusion length. The volume of distribution of gemcitabine was 50 L/m<sup>2</sup> following infusions lasting less than 70 minutes. For long infusions, the volume of distribution rose to 370 L/m<sup>2</sup>. Gemcitabine triphosphate, the active metabolite of gemcitabine, accumulates and retains in solid tumour cells _in vitro_ and _in vivo_. It is not extensively distributed to tissues after short infusions that last less than 70 minutes. It is not known whether gemcitabine crosses the blood-brain barrier, but gemcitabine is widely distributed into tissues, including ascitic fluid. In rats, placental and lacteal transfer occurred rapidly at five to 15 minutes following drug administration. |
| Clearance | Following intravenous infusions lasting less than 70 minutes, clearance ranged from 41 to 92 L/h/m<sup>2</sup> in males and ranged from 31 to 69 L/h/m<sup>2</sup> in females. Clearance decreases with age. Females have about 30% lower clearance than male patients. |
Formulation & handling
- Gemcitabine is a small molecule primarily formulated for intravenous or parenteral administration as solutions or lyophilized powders for injection.
- It exhibits high water solubility and low lipophilicity (LogP -1.5), supporting its formulation as aqueous injectable solutions.
- Stability considerations include protection from moisture in lyophilized powders and appropriate storage conditions to maintain potency prior to reconstitution.
Regulatory status
| Lifecycle | The active pharmaceutical ingredient has multiple expired patents in the United States from 2010 and 2013, with a patent extending until 2033. It is marketed in both the US and Canada, reflecting a mature market with ongoing patent protection influencing exclusivity in the US. |
|---|
| Markets | Canada, US |
|---|
Supply Chain
| Supply chain summary | The manufacturing and supply landscape for gemcitabine involves multiple originator companies, including Eli Lilly & Co., which also handles packaging. Branded products are primarily present in the US and Canadian markets. While some patents have expired, a key patent remains in force until 2033, indicating ongoing patent protection that may limit generic competition in the near term. |
|---|
Safety
| Toxicity | The oral LD<sub>50</sub> is 333 mg/kg in mice and >500 mg/kg in rats. The dermal LD<sub>50</sub> in rabbits is >1000 mg/kg. There is no known antidote for gemcitabine overdose. In a dose-escalation study, patients were administered a single dose of gemcitabine as high as 5700 mg/m<sup>2</sup> administered by intravenous infusion over 30 minutes every two weeks: main observed toxicities were myelosuppression, paresthesia, and severe rash. In the event of a suspected drug overdose, blood counts should be monitored, and patients should be provided with supportive therapy, as necessary. |
|---|
- Oral LD50 values are 333 mg/kg in mice and ›500 mg/kg in rats
- Dermal LD50 in rabbits exceeds 1000 mg/kg, indicating moderate acute toxicity
- No specific antidote is available for overdose
Gemcitabine is a type of Cytostatic antibiotics
Cytostatic antibiotics are a subcategory of pharmaceutical active pharmaceutical ingredients (APIs) that play a crucial role in the treatment of various types of cancer. These antibiotics possess powerful cytostatic or cell-inhibiting properties, which impede the growth and division of cancer cells.
Cytostatic antibiotics work by selectively targeting and inhibiting specific enzymes and proteins necessary for the replication and proliferation of cancer cells. By interrupting these vital cellular processes, these APIs effectively hinder the progression of cancer and prevent the spread of malignant cells.
One prominent example of a cytostatic antibiotic is Doxorubicin, which belongs to the anthracycline class of antibiotics. Doxorubicin functions by intercalating with DNA molecules, preventing DNA replication and inhibiting the activity of topoisomerase enzymes. These mechanisms effectively impede the growth and division of cancer cells.
Another commonly used cytostatic antibiotic is Mitomycin C. It exerts its anticancer effects by inducing DNA cross-linking, leading to the inhibition of DNA synthesis and cell division. This antibiotic is particularly effective against a variety of solid tumors.
Cytostatic antibiotics are administered in different ways, such as intravenous injection or oral consumption, depending on the specific drug. These APIs are often used in combination with other chemotherapy agents or treatment modalities to achieve optimal therapeutic outcomes.
In conclusion, cytostatic antibiotics are a vital subcategory of pharmaceutical APIs used in cancer treatment. Their ability to inhibit cell growth and division makes them essential in combating various types of cancer, ultimately improving patient outcomes.
Gemcitabine (Cytostatic antibiotics), classified under Anticancer drugs
Anticancer drugs belong to the pharmaceutical API (Active Pharmaceutical Ingredient) category designed specifically to combat cancer cells. These powerful medications play a crucial role in cancer treatment and are developed to target and destroy cancerous cells, preventing their growth and spread.
Anticancer drugs are classified based on their mode of action and can include various types such as chemotherapy drugs, targeted therapy drugs, immunotherapy drugs, and hormonal therapy drugs. Chemotherapy drugs work by interfering with the cell division process, thereby inhibiting the growth of cancer cells. Targeted therapy drugs, on the other hand, are designed to attack specific molecules or genes involved in cancer growth, minimizing damage to healthy cells. Immunotherapy drugs stimulate the body's immune system to recognize and destroy cancer cells. Hormonal therapy drugs are used in cancers that are hormone-dependent, such as breast or prostate cancer, to block the hormones that fuel cancer cell growth.
These APIs are typically synthesized through complex chemical processes in state-of-the-art manufacturing facilities. Stringent quality control measures ensure the purity, potency, and safety of these drugs. Anticancer APIs undergo rigorous testing and adhere to stringent regulatory guidelines before being approved for clinical use.
Due to their critical role in cancer treatment, anticancer drugs are in high demand worldwide. Researchers and pharmaceutical companies continually strive to develop new and more effective APIs in this category to enhance treatment outcomes and minimize side effects. The ongoing advancements in the field of anticancer drug development offer hope for improved cancer therapies and better patient outcomes.
Gemcitabine API manufacturers & distributors
Compare qualified Gemcitabine API suppliers worldwide. We currently have 24 companies offering Gemcitabine API, with manufacturing taking place in 6 different countries. Use the table below to review supplier type, countries of origin, certifications, product portfolio and GMP audit availability.
| Supplier | Type | Country | Product origin | Certifications | Portfolio |
|---|---|---|---|---|---|
| Apino Pharma Co., Ltd. | Producer | China | China | BSE/TSE, cDMF, CoA, GMP, MSDS | 229 products |
| Arch Pharmalabs | Producer | India | Unknown | CEP, CoA, FDA, GMP, USDMF | 19 products |
| Aurora Industry Co., Ltd | Distributor | China | China | BSE/TSE, CEP, CoA, GMP, ISO9001, MSDS, WC | 250 products |
| Cipla | Producer | India | India | CEP, CoA, FDA, GMP, KDMF, USDMF, WC | 164 products |
| Dr. Reddy's | Producer | India | India | BSE/TSE, CEP, CoA, FDA, GMP, JDMF, KDMF, MSDS, USDMF, WC | 170 products |
| Eli Lilly And Company | Producer | United States | United States | CEP, CoA, FDA, GMP | 5 products |
| Emcure Pharma | Producer | India | India | CoA, GMP, USDMF, WC | 80 products |
| Gonane Pharma | Producer | India | India | BSE/TSE, CoA, GMP, MSDS | 166 products |
| Hangzhou Coben Pharmaceut... | Producer | China | China | CoA | 7 products |
| Hetero Labs | Producer | India | India | CEP, CoA, FDA, GMP, JDMF, KDMF, USDMF, WC | 90 products |
| Intas Pharma | Producer | United Kingdom | United Kingdom | CEP, CoA, FDA, GMP, USDMF | 30 products |
| Jiangsu Chiatai Qingjiang | Producer | China | China | CoA, JDMF, WC | 1 products |
| Jiangsu Hansoh Pharma | Producer | China | China | CEP, CoA, GMP, JDMF, USDMF | 10 products |
| Laurus Labs | Producer | India | India | CEP, CoA, GMP, JDMF, KDMF, USDMF, WC | 50 products |
| Mac Chem Products | Producer | India | India | CoA, GMP, WC | 25 products |
| MSN Labs. | Producer | India | India | CoA, USDMF | 119 products |
| Qilu Antibiotics | Producer | China | China | CoA, JDMF | 33 products |
| SETV Global | Producer | India | India | CoA, FDA, GMP | 515 products |
| Shilpa Medicare Ltd | Producer | India | India | BSE/TSE, CEP, CoA, GMP, ISO9001, MSDS, USDMF, WC | 54 products |
| Sinoway industrial Co.,Lt... | Distributor | China | China | CoA, GMP, ISO9001, MSDS, USDMF | 757 products |
| Sun Pharma | Producer | India | India | CEP, CoA, GMP, JDMF, USDMF, WC | 219 products |
| Vidantus Alliance | Producer | Switzerland | Switzerland | CEP, CoA | 1 products |
| Yangtze River Pharma | Producer | China | China | CoA, USDMF | 2 products |
| Zhejiang Hisun Pharma | Producer | China | China | CoA, USDMF | 69 products |
When sending a request, specify which Gemcitabine API quality you need: for example EP (Ph. Eur.), USP, JP, BP, or another pharmacopoeial standard, as well as the required grade (base, salt, micronised, specific purity, etc.).
Use the list above to find high-quality Gemcitabine API suppliers. For example, you can select GMP, FDA or ISO certified suppliers. Visit our help page to learn more about sourcing APIs via Pharmaoffer.
