Oral Semaglutide and Tirzepatide: The Future of GLP-1s
- Jennifer Hardy
- 6 days ago
- 6 min read
The landscape of diabetes and obesity management is on the cusp of a significant transformation, driven by the development of oral glucagon-like peptide-1 (GLP-1) receptor agonists. That means the idea of popular weight loss drugs, like tirzepatide and semaglutide, could soon be easier to swallow literally, figuratively, and financially.
Traditionally administered via injection, GLP-1 therapies are now being formulated into pill forms, promising greater accessibility and adherence for patients. Two pharmaceutical giants, Eli Lilly and Novo Nordisk, are at the forefront of this innovation, each employing distinct strategies to bring oral GLP-1 treatments to market.
With a lot of recent headlines about oral GLP-1s, we want to get you caught up on what's happening now and what to expect in the future.
Understanding GLP-1s Impact on the Pharmaceutical Industry
GLP-1 is a naturally occurring hormone, but today’s blockbuster drugs turbocharge its effects—helping regulate blood sugar, slow digestion, and suppress appetite.
Originally developed to treat type 2 diabetes (and discovered through the help of Gila Monster saliva), the dramatic weight loss outcomes turned heads and quickly shifted demand into overdrive. These medications are now reshaping the pharmaceutical landscape, with analysts projecting the global GLP-1 market could exceed $100 billion by 2030.
What started as a diabetes breakthrough is now fueling one of the most lucrative and fast-moving revolutions in modern medicine.
Types of GLP-1 Medications
Here’s a quick breakdown of the key GLP-1 medications, who makes them, and what they’re used for as of early-2025.
Ozempic (semaglutide) – Novo Nordisk’s once-weekly injectable for type 2 diabetes. Launched in 2017, it was the first to gain mass attention for its weight loss side effects.
Wegovy (semaglutide) – Also from Novo Nordisk, this is the higher-dose version of Ozempic, FDA-approved specifically for chronic weight management.
Rybelsus (oral semaglutide) – The first oral GLP-1, approved in 2019 by Novo Nordisk for type 2 diabetes. It must be taken on an empty stomach with water.
Mounjaro (tirzepatide) – Eli Lilly’s dual agonist (GLP-1 + GIP), approved in 2022 for type 2 diabetes. It showed even greater weight loss than semaglutide in trials.
Zepbound (tirzepatide) – The weight loss version of Mounjaro, FDA-approved in 2023. Same medication, different indication.
The surge in profitability for GLP-1 drugs closely followed their approval and widespread use for weight loss. While these drugs were initially developed and prescribed for diabetes, their approval for obesity and weight management significantly expanded their market and drove unprecedented demand and revenue growth for pharmaceutical companies.
In 2018, the GLP-1 industry was valued around $57 million. By 2022, that number soared to $5.7 billion. Some estimates show it growing as high as $150 billion by 2030.
Semaglutide vs. Tirzepatide: Understanding the Differences
Semaglutide is a GLP-1 receptor agonist that mimics the incretin hormone GLP-1, enhancing insulin secretion and promoting satiety. It's available in both injectable (Ozempic, Wegovy) and oral (Rybelsus) forms.
Clinical studies have shown that semaglutide can lead to significant weight loss and improved glycemic control. Novo Nordisk is the company behind semaglutide.
Tirzepatide, on the other hand, is a dual agonist, targeting both GLP-1 and glucose-dependent insulinotropic polypeptide (GIP) receptors. We can thank the team at Eli Lilly for this one.
The dual mechanism may offer enhanced effects on insulin secretion and appetite suppression. Clinical trials have demonstrated that tirzepatide may lead to greater weight loss compared to semaglutide.
The Sticking Point of the GLP-1 Revolution
As powerful as GLP-1 medications are, they come with baggage.
The price tags are steep—often over $1,000 a month without insurance—and insurance coverage can be inconsistent, especially for those seeking them solely for weight loss.
The injectable pens, while user-friendly, are still needles, and needle aversion remains a real barrier for many. Add to that the global supply chain strain and manufacturing challenges, particularly for complex biologic formulations, and you get a high-demand treatment with limited accessibility.
Despite the overwhelming interest, not everyone can—or wants to—start a medication that involves weekly injections and tight storage guidelines.
That’s why the next phase of this revolution isn’t just exciting—it’s essential. The future of GLP-1s isn’t in the fridge. It’s in a pill.
Oral GLP-1s in Progress
We're watching the oral GLP-1 space closely, as big announcements are coming out and many wait with baited breath to see who gets there first.
To begin with, Novo Nordisk did get to the oral GLP-1 arena first. Rybelsus (oral semaglutide) got the FDA nod in 2019, approving it for type 2 diabetes. However, you don't need a crystal ball to know that it's not the future of GLP-1 pills or tablets. Here's why:
Rybelsus is not approved (and isn't on track to be approved) for weight loss.
It has strict dosing rules—you have to take it on an empty stomach with a small amount of water, then wait at least 30 minutes before eating or drinking anything else.
Weight loss outcomes weren’t as dramatic at the approved doses compared to injectables.
At the same time, Novo Nordisk announced on April 21, 2025, that they've already put an oral weight loss version of Wegovy (semaglutide) in front of U.S. regulators. This came after the OASIS 1 phase 3A trial in 2023. While the April announcement was a bit cryptic, we're expecting to learn more on May 7.
It's important to note that in that same timeframe, semaglutide was in a global shortage crisis. With the oral semaglutide (and yet unnamed medication for weight loss), supply chain concerns persist since the oral dose (up to 50 mg daily) is much higher than the injectable version.
Eli Lilly has been a prominent figure in the GLP-1 arena with its injectable medications, Mounjaro (tirzepatide) for type 2 diabetes and Zepbound for weight management. Building on this foundation, Lilly is developing orforglipron, a novel oral GLP-1 receptor agonist.
Unlike peptide-based injectables, orforglipron is a small-molecule compound, which simplifies manufacturing and storage, as it doesn't require refrigeration. Lilly plans to submit orforglipron for regulatory approval for weight management by the end of 2025 and for diabetes in 2026, positioning it as a potentially transformative, needle-free option in the obesity and diabetes market.
Understanding Big Pharma: Why Two Iterations of the Same Medication?
Companies make separate GLP-1 drugs for diabetes and weight loss because people with these conditions need different amounts of medicine, and the goals of treatment are not the same.
For diabetes, the main job of the drug is to lower blood sugar, while for weight loss, the drug is given at a higher dose to help people lose more weight safely and effectively.
Having separate drugs lets doctors give the right dose for each health concern, helps keep people safe from side effects, and makes it easier for insurance companies and the FDA to approve and pay for the right treatment for each person.
Other Companies Working on Oral GLP-1s
It’s hard to be a pharmaceutical company and ignore the massive impact of the GLP-1 space—but it’s also hard to jump in. Patent protections on semaglutide and tirzepatide lock out competitors for now, meaning most companies are either licensing, racing to develop next-gen alternatives, or waiting for a window to open.
The market is booming, but access to the core molecules remains tightly guarded. With the FDA, Lilly, and Novo Nordisk cracking down on compounding pharmacies now that the shortage is over, the race of next-gen weight is on.
Let's look at some other efforts being made to turn GLP-1s into oral options.
Pfizer was working on danuglipron, an oral GLP-1 receptor agonist, with a once-daily formulation. The company stopped development in 2025 after a clinical trial participant experienced a potential drug-induced liver injury, which resolved after stopping the medication.
Viking Therapeutics is working on VK2735, which has both oral and injectable versions; the oral formulation is in Phase II trials.
Jiangsu Hengrui (China) has HRS-9531, a dual GLP-1/GIP receptor agonist in Phase III trials.
Metsera and other smaller biotech firms are also entering the space, with early-stage oral GLP-1 candidates and manufacturing partnerships.
Industry reports indicate there are more than 60 oral GLP-1 receptor agonists in active development globally, with at least four in Phase III trials as of late 2024.
How would having an oral (pill) version of a GLP-1 medication change your interest in taking it?
Not interested in the GLP-1 hype
I'd be more open to a pill form
I would switch from injections to the pill
I wouldn't change a thing
The Race to First in the Future of Oral GLP-1s
Developing oral GLP-1 drugs matters because they’re easier for patients to take, especially those who dislike injections. Pills improve adherence, expand access, and open the door to people who wouldn’t consider injectables. They’re also potentially cheaper to make and distribute, giving companies a cost advantage and a bigger slice of the growing diabetes and obesity market.
Who will get there first? It remains to be seen. We will keep tracking the topic and look for announcements in May 7 from Novo Nordisk and the FDA as they review orforglipron. Sign up for our newsletter and breaking news alerts to stay in the know.
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