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. On September 29, 2026, Innsbruck-based Cyprumed said MSD had started the first human trial of a peptide formulated with its oral tablet technology, under a 2025 agreement worth up to $493 million.
Stories here cover platform readouts and the deals around them. See #oral-peptides and #drug-delivery for related threads.
Johnson & Johnson said on October 9, 2026, at the Fall Clinical Dermatology Conference, that in the Phase 3 ICONIC-LEAD trial of its oral IL-23 receptor-blocking peptide Icotyde (icotrokinra) in 684 people aged 12 and older with moderate to severe plaque psoriasis, at least 70% of treated patients had clear or almost clear skin, at least 44% had completely clear skin by PASI 100, and at least 72% reached PASI 90 at week 112. Among people who reached PASI 90, stopped the drug at week 24, and later restarted it, 85% regained that response within 24 weeks. The release does not say how patients who left the study were counted, and J&J reported no new safety signals.
Viking Therapeutics said on October 6, 2026 that it had started Part 2 of its maintenance study of VK2735, its GLP-1 and GIP dual agonist. About 195 adults with obesity who took weekly VK2735 injections or placebo for 21 weeks in Part 1 are being randomized to daily or weekly oral doses, monthly or every-other-week injections, or placebo through week 33, with safety, tolerability, and drug levels as the main goals and weight change as an exploratory measure. Viking expects results in 2027; its two Phase 3 VANQUISH trials, with about 4,500 and 1,000 participants, are fully enrolled.
Researchers at Lembas Bio and Tel Aviv University reported in ACS Nutrition Science on October 6, 2026 an AI-guided design pipeline, built on AlphaFold2 structural modeling, for peptides that act on nutrient-sensing receptors of the gut cells that release the hormone GLP-1. After four rounds of design and screening, lead peptides raised GLP-1 secretion more than 27-fold in a mouse gut cell line, exceeding an optimized small-molecule GLP-1 secretagogue, and 28 days of oral dosing reduced food intake and body weight in diet-induced obese rats, with semaglutide as an active comparator. The authors present the work as a route to nutritional ingredients, and the results so far come from cells and rats.
Johnson & Johnson reported two-year results on Friday, October 2, 2026, at the EADV Congress in Vienna from the Phase 3 ICONIC-TOTAL trial of Icotyde (icotrokinra), a once-daily oral peptide that blocks the IL-23 receptor, in 311 people aged 12 and older with psoriasis on the scalp, genitals, hands, or feet (208 on icotrokinra and 103 on placebo, who switched to the drug at week 16). Among icotrokinra-treated patients, the share with clear or almost clear skin rose from 57% at week 16 to 70% at week 112, and 60% of those with scalp psoriasis, 89% with genital psoriasis, and 63% with hand or foot psoriasis had complete clearance at those sites. Missing data after week 52 were handled with multiple imputation, and J&J reported no new safety signals.
Innsbruck-based Cyprumed announced on Tuesday, September 29, 2026 that MSD (Merck & Co.) has begun a Phase 1 trial of one of its proprietary drug candidates formulated with Cyprumed's oral delivery technology, the first time the technology has been tested in people; the candidate was not disclosed. Cyprumed's tablet formulations are designed to let therapeutic peptides, including GLP-1 analogs, macrocycles, and mini-proteins, be absorbed when swallowed, using approved excipients. The trial start triggers a milestone payment under the companies' April 2025 non-exclusive license and option agreement to develop oral versions of MSD's peptides, under which Cyprumed can receive up to $493 million.
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.