Oral peptide as a tag (singular form) covers the same field as #oral-peptides — the formulation chemistry that makes peptide drugs survive the gut and cross the intestinal epithelium at therapeutic dose.
Key programs: oral semaglutide and oral Wegovy (SNAC-based salt-permeation enhancers), Vivtex's permeability platforms, J&J's oral icotrokinra in plaque psoriasis, and the small-molecule oral alternatives (orforglipron / Foundayo) that bypass peptide-bioavailability constraints.
Stories here cover platform readouts and the deals around them. See #oral-peptides and #drug-delivery for related threads.
General Bio, a developer of oral GLP-1s and other peptides, has raised $7.4 million and is pursuing a larger follow-on funding round, CEO David Kim told Axios Pro Biotech Deals in an exclusive report published Monday July 20, 2026. The company is one of several new-generation oral peptide startups seeking to compete against the established oral-peptide market, which now spans Novo Nordisk's Wegovy pill (oral semaglutide 25 mg, launched January 2026, over 3 million US prescriptions by June), Merck's LIPFENDRA (enlicitide, oral macrocyclic peptide PCSK9 inhibitor FDA-approved July 16, 2026), and MindRank AI's MDR-001 (AI-designed oral small-molecule GLP-1RA in Phase 3 MOBILE trial in China, $52M Series B closed July 9). The oral peptide category economics are shaped by macrocyclic peptide chemistry (Merck's LIPFENDRA approach) that allows survival through the gastrointestinal tract, permeation-enhancer formulations (Novo's SNAC technology for oral semaglutide), and next-generation delivery platforms including Rani Therapeutics' RaniPill capsule (July 9 collaboration announced with China's PegBio). Seed-stage entrants like General Bio typically position on proprietary chemistry or delivery mechanisms that could enable next-generation peptides beyond the current oral GLP-1 wave.
Merck LIPFENDRA (enlicitide) commercial-launch details firmed up in the days following Thursday July 16, 2026 FDA approval. List price: $10.50 per tablet, or $315 per 30-day supply before insurance discounts, manufacturer support, or pharmacy benefit adjustments. Distribution channel: standard retail and mail-order pharmacies under the pharmacy benefit, which contrasts with Novartis Leqvio (inclisiran) that runs through the medical benefit due to healthcare-provider subcutaneous administration. Expected pharmacy availability: within weeks of approval. The pharmacy benefit pathway matters for real-world access because it eliminates the buy-and-bill logistics that have slowed injectable PCSK9 adoption (Repatha, Praluent, Leqvio) and puts LIPFENDRA on the same pharmacy shelf as statins and cheaper oral non-statin drugs like Nexletol (bempedoic acid) and Zetia (ezetimibe). The macrocyclic peptide's ability to survive gastrointestinal enzymes is what allows the oral delivery model that unlocks the pharmacy-benefit distribution advantage.
The US Food and Drug Administration approved Merck's LIPFENDRA (enlicitide) 20 mg tablets Thursday July 16, 2026 as an adjunct to diet and exercise to reduce low-density lipoprotein cholesterol (LDL-C) in adults with hypercholesterolemia, including heterozygous familial hypercholesterolemia (HeFH). LIPFENDRA is a novel macrocyclic peptide and becomes the first FDA-approved oral PCSK9 inhibitor. In the registrational Phase 3 CORALreef Lipids trial, enlicitide achieved a 56% placebo-adjusted LDL-C reduction; in CORALreef HeFH the reduction was 59%. Every other FDA-approved PCSK9 inhibitor (Amgen's Repatha/evolocumab, Regeneron/Sanofi's Praluent/alirocumab) is delivered by subcutaneous injection every two to four weeks; enlicitide is the first approved as a once-daily oral tablet. Merck priced LIPFENDRA at $315 per month list price, roughly one-third the approximately $700-900/month list prices of the injectable PCSK9 antibodies. The approval extends the macrocyclic peptide platform's clinical validation and opens a new oral chapter for a drug class that had been injectable-only since the first FDA approvals in 2015.
South Korea's D&D Pharmatech and LG AI Research announced June 17 a joint development agreement for AI-designed next-generation oral peptide drugs. LG AI Research will use its EXAONE Discovery pharmaceutical AI platform, which analyzes disease-causing protein structures to design optimal peptide sequences, while D&D contributes its oral peptide delivery experience and obesity-pipeline programs. D&D's shares closed up 16.59% on the announcement. The deal extends D&D's late-cycle pipeline momentum, following the April 2026 $1.3M Pfizer research contract on oral obesity peptides after Pfizer's Metsera acquisition, and the June ADA showcase of Korean monthly-GLP-1 programs.
Entera Bio (Nasdaq: ENTX) presented full single-tablet EB613 results on June 14 at ENDO 2026 in Chicago as a late-breaking oral. The single-tablet EB613 achieved a comparable pharmacokinetic and pharmacodynamic profile to Forteo (injectable teriparatide) and to the multi-tablet EB613 used in Entera's earlier Phase 2 study in postmenopausal women with osteoporosis. On the administration-experience quality-of-life questionnaire, 14 of 15 study participants preferred the single tablet to the multi-tablet format, and all 15 preferred the daily oral EB613 to the daily injection. Entera plans to advance the single-tablet formulation into the Phase 3 trial in 750 postmenopausal women starting late 2026, with topline expected H2 2028.
Entera Bio (Nasdaq: ENTX) confirmed that its first-in-class oral PTH(1-34) tablet EB613 was selected for a late-breaking oral presentation at ENDO 2026 covering single-tablet data ahead of the 750-patient Phase 3 trial set to start late 2026 in postmenopausal osteoporosis. EB613 applies Entera's N-Tab oral-peptide delivery platform to teriparatide (the active ingredient in Forteo). On the obesity side, Entera will present preclinical PK/PD data on EB618, a first-in-class oral dual GLP-1/glucagon receptor agonist, in non-human primates on Saturday June 13 12:15-1:45 PM CT. The ENDO slot extends Entera's spring narrative beyond the Q1 2026 Phase 3 plan first disclosed in May.
Entera Bio reported Q1 2026 May 8 with $20.4M cash and an updated Phase 3 plan for EB613, an oral once-daily PTH(1-34) tablet that would be the first oral osteoanabolic for postmenopausal osteoporosis. The streamlined Phase 3 protocol — submitted to the FDA in March — covers 750 postmenopausal women with primary endpoint of total hip BMD change from baseline at month 12. Trial initiation is targeted for late 2026, with topline H2 2028 — roughly one year earlier than previously guided. The molecule applies Entera's N-Tab oral peptide platform to teriparatide, the active ingredient in Forteo. The Phase 2 dose-ranging study in 161 patients met primary (PD/bone-turnover biomarker) and secondary (BMD) endpoints.
Joelle Pelletier's perspective in Science (volume 392, pages 582-583, published online May 8) accompanies the Merck enlicitide biocatalytic synthesis paper and frames the enzyme-cascade route — engineered enzymes plus chromatography-free crystallization to cut step count by more than half — as a template that goes well beyond enlicitide. The piece argues that the limiting step for oral macrocyclic peptide therapeutics has been the manufacturing cost of multi-step protected-residue chemistry, not pharmacology or pharmacokinetics; biocatalysis collapses the cost curve and unlocks a pipeline of oral peptides at large molecular weights that have been quietly stuck in preclinical or Phase 1 economics. The framing matters as enlicitide (oral PCSK9 inhibitor with 57% LDL-C reduction at 24 weeks) heads toward NDA filing.
TIDES USA 2026 opens in Boston May 11-14 with a featured presentation on Chugai's LUNA18 (paluratide), an N-alkyl-rich cyclic undecapeptide oral KRAS inhibitor. The corresponding paper in Organic Process Research & Development describes a convergent 24-step liquid-phase synthesis route delivering kilogram-scale GMP material at >98.5% purity and >30% overall yield. LUNA18 binds KRAS, NRAS, and HRAS mutants plus wildtype, inhibiting the inactive-state RAS-GEF protein-protein interaction; it achieves 21-47% oral bioavailability without special formulation. The molecule is in Phase 1 monotherapy and combination-with-cetuximab dose escalation. LUNA18's chemistry is a milestone for the oral-cyclic-peptide-against-intracellular-targets thesis that Bicycle Therapeutics, Circle Pharma, and Unnatural Products are advancing through different platform architectures.
Merck scientists published in Science a convergent biocatalytic synthesis of enlicitide decanoate, an investigational oral PCSK9 inhibitor and macrocyclic peptide. A tailored suite of engineered enzymes catalyzes selective peptide fragment formation, coupling, and macrocyclization in a protecting-group-free sequence; combined with chromatography-free crystallizations, the route reduces step count by more than half versus prior state-of-the-art methods. Enlicitide is in Phase 3 (CORALreef, with –55.8% LDL-C reported earlier in 2026) and would be the first oral PCSK9 inhibitor if approved. The paper matters beyond enlicitide: protein-engineering-led cascades shift the cost basis for any large macrocyclic peptide program facing peptide-CDMO bottlenecks.
OrbiMed-incubated Pinnacle Medicines is featured at the Boston peptide summit highlighting its oversubscribed $89M Series B financing (closed March 26) for advancing oral peptide therapeutics designed to match the efficacy of injectable biologics. Lead programs target asthma, COPD, immunology, and inflammation — distinct from the GLP-1 obesity focus dominating peptide headlines. The platform combines proprietary peptide stabilization with oral-bioavailability engineering, positioning Pinnacle as one of the most differentiated non-GLP-1 oral peptide developers in the current pipeline.
Merck's investigational oral macrocyclic peptide PCSK9 inhibitor demonstrated significantly greater LDL-C reductions at 8 weeks vs guideline-recommended oral non-statin therapies, delivering injectable-level cholesterol lowering in pill form.
Oral peptide icotrokinra delivered complete skin clearance through week 52 with a strong safety profile in the ICONIC-ADVANCE trials, presented at the American Academy of Dermatology meeting.