MedPath

Bupivacaine

Generic Name
Bupivacaine
Brand Names
Exparel, Kenalog, Marbeta, Marcaine, Marcaine With Epinephrine, Marvona Suik, P-Care M, P-Care MG, P-care, Posimir, Readysharp Anesthetics Plus Ketorolac, Readysharp-A, Readysharp-p40, Readysharp-p80, Sensorcaine, Sensorcaine With Epinephrine, Vivacaine, Xaracoll, Exparel liposomal
Drug Type
Small Molecule
Chemical Formula
C18H28N2O
CAS Number
38396-39-3
Unique Ingredient Identifier
Y8335394RO
Background

Bupivacaine is a widely used local anesthetic agent.

Indication

As an implant, bupivacaine is indicated in adults for placement into the surgical site to produce postsurgical analgesia for up to 24 hours following open inguinal hernia repair.

Bupivacaine, in liposome suspension, is indicated in patients aged 6 years and older for single-dose infiltration to produce postsurgical local analgesia. In adults, it is also indicated as an interscalene brachial plexus nerve block to produce postsurgical regional analgesia.

Bupivacaine, in combination with meloxicam, is indicated for postsurgical analgesia in adult patients for up to 72 hours following foot and ankle, small-to-medium open abdominal, and lower extremity total joint arthroplasty surgical procedures.

Bupivacaine, alone or in combination with epinephrine, is indicated in adults for the production of local or regional anesthesia or analgesia for surgery, dental and oral surgery procedures, diagnostic and therapeutic procedures, and for obstetrical procedures. Specific concentrations and presentations are recommended for each type of block indicated to produce local or regional anesthesia or analgesia. Finally, its use is not indicated in all blocks given clinically significant risks associated with use.

Associated Conditions
Acute Gouty Arthritis, Adrenocortical Insufficiency, Alopecia Areata (AA), Ankylosing Spondylitis (AS), Berylliosis, Bullous dermatitis herpetiformis, Congenital Adrenal Hyperplasia (CAH), Congenital Hypoplastic Anemia, Dermatomyositis (DM), Discoid Lupus Erythematosus (DLE), Edema of the cerebrum, Epicondylitis, Hemolytic Anemia, Hypercalcemia caused by Cancer, Keloids Scars, Leukemias, Mycosis Fungoides (MF), Necrobiosis lipoidica diabeticorum, Ocular Inflammation, Ophthalmia, Sympathetic, Osteoarthritis (OA), Pain, Labor, Polymyositis, Postoperative pain, Psoriatic Arthritis, Psoriatic plaque, Pure Red Cell Aplasia, Regional Enteritis, Rheumatoid Arthritis, Secondary thrombocytopenia, Stevens-Johnson Syndrome, Synovitis, Systemic Lupus Erythematosus, Temporal Arteritis, Trichinosis, Tuberculous Meningitis, Ulcerative Colitis, Uveitis, Acute Bursitis, Acute Idiopathic Nephrotic Syndrome, Acute Lupus Erythematosus, Acute Multiple sclerosis, Acute Rheumatic heart disease, unspecified, Acute nonspecific tenosynovitis, Cystic tumors of aponeurosis, Cystic tumors of tendon, Disseminated Pulmonary Tuberculosis (TB), Exfoliative erythroderma, Inflammatory lesions of granuloma annulare, Inflammatory lesions of lichen planus, Inflammatory lesions of lichen simplex, Non-suppurative Thyroiditis, Permphigus, Severe Allergic Reactions
Associated Therapies
General Anesthesia, Local Anaesthesia therapy, Regional nerve block therapy

Pacira BioSciences Secures Future of Exparel with Strategic Patent Settlement Agreement

• Pacira BioSciences has reached a settlement agreement with Fresenius, Jiangsu Hengrui Pharmaceuticals, and eVenus Pharmaceuticals regarding patents for its pain management drug Exparel, protecting market exclusivity until 2030. • Under the agreement, Fresenius will begin limited-volume sales of generic bupivacaine liposome injectable suspension in early 2030, with gradual market share increases reaching the high thirties percent by the final years of the agreement. • The settlement strategically preserves Pacira's market dominance for its lead drug Exparel for nearly a decade before allowing controlled generic entry, significantly extending protection beyond potential patent challenges.

Pacira BioSciences Settles EXPAREL Patent Litigation with Fresenius Kabi, Securing Market Exclusivity Until 2030

• Pacira BioSciences has reached a settlement with Fresenius Kabi and other companies regarding patent litigation for its non-opioid pain therapy EXPAREL, allowing limited generic entry beginning in early 2030. • The agreement permits Fresenius to sell volume-limited amounts of generic bupivacaine liposome injectable suspension starting with high-single-digit percentages, gradually increasing to a maximum in the high thirties by the final years. • Unlimited generic production by Fresenius will not be permitted until 2039, significantly before EXPAREL's last patent expiration in 2044, allowing Pacira to maintain market dominance for its flagship product.

Pacira BioSciences Advances Novel Gene Therapy for Knee Osteoarthritis with First Patient Dosed in Phase 2 Trial

• Pacira BioSciences has dosed the first patient in its Phase 2 ASCEND study evaluating PCRX-201, a locally administered gene therapy designed to treat osteoarthritis of the knee by boosting anti-inflammatory protein production. • The innovative therapy utilizes Pacira's proprietary high-capacity adenovirus vector platform and features an inducible promoter that activates IL-1Ra expression during inflammation and deactivates when inflammation subsides. • In previous Phase 1 trials, PCRX-201 demonstrated sustained pain relief for at least two years across all osteoarthritis severity levels, with topline results from the current two-part study expected by late 2026.

Virpax's Probudur Shows Promise in Pain Management Studies, Advancing Toward IND Application

• Virpax Pharmaceuticals' non-opioid pain management candidate Probudur demonstrated positive results in a U.S. Army-performed preclinical study, showing effective reduction in incision-induced pain behaviors compared to competitors. • The long-acting liposomal bupivacaine formulation exhibited safety in a beagle dog dose range finding study, with doses up to 90 mg/kg well-tolerated and no adverse effects reported. • Preclinical data indicates Probudur provides extended pain control for up to 96 hours, with potential to significantly reduce or eliminate post-surgical opioid requirements in approved indications.

Larsucosterol Shows Promising 90-Day Mortality Reduction in Phase 2b Alcohol-Associated Hepatitis Trial

• Phase 2b AHFIRM trial results published in NEJM Evidence demonstrate larsucosterol reduced 90-day mortality by up to 41% in alcohol-associated hepatitis patients compared to placebo. • U.S. patient subgroup analysis revealed even more substantial mortality reductions of 57-58% with both 30mg and 90mg doses, showing strong statistical significance. • The drug demonstrated a favorable safety profile with treatment-emergent adverse events comparable to placebo, marking a potential breakthrough for a condition with no FDA-approved therapies.

Evorpacept Shows Promise in HER2-Positive Gastric Cancer: Updated ASPEN-06 Data

• ALX Oncology's ASPEN-06 Phase 2 trial evaluates evorpacept, a CD47-blocker, in HER2-positive advanced gastric cancer patients who have been previously treated. • Updated data from the ASPEN-06 trial were presented at the 2025 ASCO Gastrointestinal Cancers Symposium (ASCO GI). • The virtual event hosted by ALX Oncology on January 23, reviewed the ASPEN-06 data, focusing on evorpacept's potential in immuno-oncology. • The ASPEN-06 trial is a phase 2/3 study of evorpacept in patients with HER2-overexpressing gastric/gastroesophageal cancer.

Pacira Receives FDA Clearance for Iovera System to Treat Chronic Back Pain

• Pacira BioSciences has received FDA clearance for its Iovera system with a longer-needle Smart Tip to treat chronic low back pain, offering a drug-free alternative. • The Iovera system uses cryoneurolysis to temporarily halt nerve signals, providing pain relief that can last for months, and has shown benefits in a pilot study. • This approval expands the use of the Iovera system, already used for knee, hip, shoulder, and ankle pain, to address the significant health issue of chronic low back pain. • Pacira's focus on non-opioid pain therapies is further strengthened by this clearance, complementing their existing products like EXPAREL and ZILRETTA.

FDA Advisers Reject New Use for Pacira Nerve Block

FDA advisers have voted against the expanded use of Pacira Pharmaceuticals' pain therapy Exparel as a nerve block after surgery, casting doubt on its approval for this new indication.

FDA Approves Heron Therapeutics' Zynrelef Vial Access Needle for Postoperative Pain Management

• The FDA has approved Heron Therapeutics' Prior Approval Supplement Application for the Zynrelef Vial Access Needle (VAN). • The VAN simplifies aseptic preparation and significantly reduces Zynrelef's withdrawal time to 20-45 seconds. • Expected to launch in Q4 2024, the VAN aims to enhance safe use, increase adoption, and improve the preparation process of Zynrelef. • Zynrelef is a dual-acting local anesthetic combining bupivacaine and meloxicam, designed to reduce postoperative pain for up to 72 hours.

DURECT's Larsucosterol Shows Promise in Alcohol-Associated Hepatitis Treatment

• DURECT Corporation's larsucosterol demonstrates potential in treating alcohol-associated hepatitis (AH) by reducing mortality rates in U.S. patients. • A Phase 3 trial, agreed upon with the FDA, will assess larsucosterol's efficacy with a 90-day survival primary endpoint, aiming for topline data within two years. • Larsucosterol targets DNA methyltransferases, epigenetic enzymes linked to hypermethylation in AH, offering a novel approach to managing the condition. • Data from the AHFIRM Phase 2b trial supports the Phase 3 design, showing significant mortality reduction with larsucosterol in U.S. patients.

FDA Nears Decisions on Key Therapies for Gastroparesis, Niemann-Pick Disease, Schizophrenia, COPD, Mesothelioma, and Post-Surgical Pain

• The FDA is expected to decide on Vanda Pharmaceuticals' tradipitant for gastroparesis by September 18, potentially offering a novel NK-1R antagonist treatment option. • Zevra Therapeutics awaits a verdict by September 21 on arimoclomol for Niemann-Pick disease type C, an ultrarare neurodegenerative disorder with no approved therapies. • A decision is anticipated by September 26 on Bristol Myers Squibb's KarXT for schizophrenia, representing a new pharmacological approach targeting muscarinic receptors.

FDA Nears Decisions on Vanda, Zevra, Heron, Merck, BMS, Sanofi/Regeneron

• Vanda Pharmaceuticals awaits FDA decision on tradipitant for gastroparesis, a condition affecting millions in the U.S., with a verdict expected by September 18. • Zevra Therapeutics anticipates potential approval of arimoclomol for Niemann-Pick disease type C (NPC) by September 21, following positive advisory committee support. • The FDA is set to decide on Heron Therapeutics' extended-release needle for Zynrelef by September 23, designed to simplify drug preparation and administration. • Merck seeks approval for Keytruda in pleural mesothelioma, with a decision due September 25, based on Phase II/III KEYNOTE-483 trial data showing improved survival. • Bristol Myers Squibb awaits FDA decision on KarXT for schizophrenia by September 26, potentially offering a novel mechanism of action targeting muscarinic receptors. • Sanofi and Regeneron anticipate a decision on Dupixent for COPD by September 27, supported by Phase III BOREAS and NOTUS trials demonstrating reduced exacerbations.

Vertex's Non-Opioid Pain Medication VX-548 Shows Promise Amid Clinical and Reimbursement Challenges

• Vertex Pharmaceuticals' VX-548, a non-opioid pain medication, has demonstrated statistically significant pain improvement compared to placebo in late-stage trials. • While VX-548 shows promise, it did not outperform a combination of acetaminophen and hydrocodone in post-surgical pain relief, highlighting the challenge in matching opioid efficacy. • The development of non-opioid pain treatments faces clinical hurdles, as seen with previous failures like tanezumab due to safety concerns and limited effectiveness. • Non-opioid pain medications, even when approved, often encounter reimbursement barriers from insurers, who may favor cheaper, generic opioid options.

Ensysce Biosciences Advances Novel Analgesics PF614 and PF614-MPAR Towards Phase 3 Trials

• Ensysce Biosciences is advancing PF614, an extended-release oxycodone, towards Phase 3 trials after positive clinical trial data and FDA discussions. • Clinical data indicates PF614 is bioequivalent to OxyContin but with a longer half-life, potentially improving pain relief with twice-daily dosing. • PF614-MPAR, designed with MPAR technology, aims to prevent overdoses by reducing oxycodone release when multiple doses are consumed. • Ensysce is also exploring BupiZenge, a bupivacaine lozenge for oral mucositis pain, to diversify its pain management portfolio.

Novartis' Sandoz Partners with Pear Therapeutics to Combat Substance Use Disorders with Digital Solutions

• Sandoz, a Novartis division, has partnered with Pear Therapeutics to commercialize reSET, the first FDA-approved mobile medical application for treating substance use disorders. • The collaboration includes development of reSET-O, a specialized digital therapeutic for opioid use disorder patients undergoing buprenorphine treatment. • This strategic partnership expands upon an existing collaboration between Novartis and Pear to develop digital therapeutics for schizophrenia and multiple sclerosis patients.
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